A series of substituted pyrazoline derivatives 5(a-c) have been synthesized by the reaction of substituted chalcones 4(a-c) with isatinhydrazide. The starting materials, chalcones were prepared by clasien schimidt condensation of appropriate 1-hydroxy-2-acetonaphthone with substituted aldehydes in the presence of sodium hydroxide and in poly ethylene glycol (PEG-400). The structures of the synthesized compounds were confirmed by IR, 1HNMR & Mass spectral data. The synthesized compounds were screened for Antioxidant Activity by DPPH method.
The document describes the synthesis and characterization of new imidazole derivatives derived from D-erythroascorbic acid. D-erythroascorbic acid was modified through multi-step reactions to yield Schiff bases containing heterocyclic units like 1,3,4-oxadiazole and 1,3,4-thiadiazole. These Schiff bases were further derivatized to yield N-acyl, thiourea, and imidazole compounds. The structures of the synthesized compounds were characterized using techniques like elemental analysis, FTIR, NMR, and mass spectrometry. The compounds exhibited good antibacterial activity against Escherichia coli and Staphylococcus aureus.
This document describes a novel method for synthesizing highly functionalized 3,4-dihydropyrimidin-2(1H)-ones (DHPMs) through 1,4-addition of nucleophiles onto pyrimidin-2(1H)-ones. Ceric ammonium nitrate (CAN) is used as a catalyst to promote the 1,4-addition reaction of indoles and other nucleophiles with pyrimidin-2(1H)-ones to form novel DHPMs in good yields. A variety of substituted indoles undergo regioselective 1,4-addition to form functionalized 4-indolyl-DHPMs. Pyrrole and sodium boroh
Synthesis, characterization, in vitro cytotoxic and antioxidant activities of...ijperSS
ABSTRACT
A series of novel (Z)-3-(2-(4-(2-oxo-2H-chromen-3-yl) thiazol-2-yl-)hydrazono)indolin-2-one (8a-8d, 9) were synthesized with various substituted indole derivatives. Structures of the newly synthesized compounds were elucidated by FT-IR, 1H-NMR, 13C-NMR and API-ES Mass spectral data. The in vitro cytotoxic activities of the complexes measurement against the human cancer T-lymphocyte cell lines. In vitro evaluation of these title complexes revealed cytotoxicity from 6.8-18µg/mL against CEM, 9.2-21µg/mL against L1210, 10-19µg/mL against Molt4/C8, 8-12µg/mL against HL60 and 8-16µg/mL against BEL7402. Coumarin derivatives 8c and 8d showed that quite significant anticancer activities. The antioxidant activity of the synthesized compounds was evaluated by DPPH scavenging method. Compounds 8c, 8d and 9 showed significant antioxidant activity compared with that of standard drug, ascorbic acid.
Key words: Coumarin, DPPH, Cytotoxic activity.
Simple Synthesis of Some Novel Polyfunctionally Derivatives of 2H-Coumarin-2-...IOSRJAC
Compound (2) was prepared from the reaction of ethyl-2-oxo-2H-coumarin-3-carboxylate (1) with ethylcyanoacetate in ethanol containing a catalytic amount of piperidine as catalyst. Compound (2) is the key intermediate for the synthesis of several series of new compounds such as ((pyrimidine, tetrazine, piperidine, oxazepine)-2H-coumarin-2-one derivatives by reaction with selected reagents such as urea, cyanoacetamide, cyanoacetohydrazide, orthoaminophenol and 5-aminotriazole.
Synthesis and Characterization of Schiff Base from Aromatic Amine and Aromati...ijtsrd
The synthesis of Schiff base From Aromatic Amine And Aromatic P Nitro benzaldehyde was performed by a novel method of stirring followed by the addition of p nitro benzaldehydeandm nitro aniline 0.02M . Characterization of the synthesized compounds, determination of purity and identity of the compounds using following spectroscopic and chromatographic techniques Solubility, Thin Layer Chromatographic studies, Ultra Violet studied rotational and vibrational studies FT IR studies. The compounds were investigated for their Antimicrobial activity by cup plate method. Compound1 nitro 4 1 imino,4 nitrophenyl benzene was found to be the most active according to pharmacological evaluation exhibited antimicrobial. Ms. Chetana D. Patil | Mr. Digamber N. Bhosale | Ms. Smita P. Bedis "Synthesis and Characterization of Schiff Base from Aromatic Amine and Aromatic P-Nitro Benzaldehyde" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-3 | Issue-5 , August 2019, URL: https://www.ijtsrd.com/papers/ijtsrd26401.pdfPaper URL: https://www.ijtsrd.com/pharmacy/medicinal-chemistry/26401/synthesis-and-characterization-of-schiff-base-from-aromatic-amine-and-aromatic-p-nitro-benzaldehyde/ms-chetana-d-patil
This document summarizes the synthesis of new C-2, C-3 substituted heterocyclic derivatives of L-ascorbic acid and their characterization and evaluation of bacterial activity. Specifically, it describes the multi-step synthesis of Schiff bases and 1,3-oxazepine derivatives from L-ascorbic acid, including protection of hydroxyl groups, esterification, hydrazide formation, Schiff base formation with substituted benzaldehydes, and Diels-Alder reaction with phthalic anhydride to form 1,3-oxazepines. The synthesized compounds were characterized using melting point, FTIR, and 1H NMR spectroscopy and tested for antibacterial activity against gram-positive and
IJERA (International journal of Engineering Research and Applications) is International online, ... peer reviewed journal. For more detail or submit your article, please visit www.ijera.com
The document describes a new synthesis method for bisacodyl, a substituted diphenyl(2-pyridyl)methane derivative that has laxative activity. The key steps involve migrating a 2-pyridacyl group from phenyl pyridine-2-carboxylate to form 4-hydroxyphenyl(2-pyridyl) ketone when reacted with aluminum chloride, then condensing this intermediate with phenol in the presence of phosphoric acid to form the target bisacodyl compound. This new method uses more readily available pyridine-2-carboxylic acid as a starting material compared to existing synthesis routes
The document describes the synthesis and characterization of new imidazole derivatives derived from D-erythroascorbic acid. D-erythroascorbic acid was modified through multi-step reactions to yield Schiff bases containing heterocyclic units like 1,3,4-oxadiazole and 1,3,4-thiadiazole. These Schiff bases were further derivatized to yield N-acyl, thiourea, and imidazole compounds. The structures of the synthesized compounds were characterized using techniques like elemental analysis, FTIR, NMR, and mass spectrometry. The compounds exhibited good antibacterial activity against Escherichia coli and Staphylococcus aureus.
This document describes a novel method for synthesizing highly functionalized 3,4-dihydropyrimidin-2(1H)-ones (DHPMs) through 1,4-addition of nucleophiles onto pyrimidin-2(1H)-ones. Ceric ammonium nitrate (CAN) is used as a catalyst to promote the 1,4-addition reaction of indoles and other nucleophiles with pyrimidin-2(1H)-ones to form novel DHPMs in good yields. A variety of substituted indoles undergo regioselective 1,4-addition to form functionalized 4-indolyl-DHPMs. Pyrrole and sodium boroh
Synthesis, characterization, in vitro cytotoxic and antioxidant activities of...ijperSS
ABSTRACT
A series of novel (Z)-3-(2-(4-(2-oxo-2H-chromen-3-yl) thiazol-2-yl-)hydrazono)indolin-2-one (8a-8d, 9) were synthesized with various substituted indole derivatives. Structures of the newly synthesized compounds were elucidated by FT-IR, 1H-NMR, 13C-NMR and API-ES Mass spectral data. The in vitro cytotoxic activities of the complexes measurement against the human cancer T-lymphocyte cell lines. In vitro evaluation of these title complexes revealed cytotoxicity from 6.8-18µg/mL against CEM, 9.2-21µg/mL against L1210, 10-19µg/mL against Molt4/C8, 8-12µg/mL against HL60 and 8-16µg/mL against BEL7402. Coumarin derivatives 8c and 8d showed that quite significant anticancer activities. The antioxidant activity of the synthesized compounds was evaluated by DPPH scavenging method. Compounds 8c, 8d and 9 showed significant antioxidant activity compared with that of standard drug, ascorbic acid.
Key words: Coumarin, DPPH, Cytotoxic activity.
Simple Synthesis of Some Novel Polyfunctionally Derivatives of 2H-Coumarin-2-...IOSRJAC
Compound (2) was prepared from the reaction of ethyl-2-oxo-2H-coumarin-3-carboxylate (1) with ethylcyanoacetate in ethanol containing a catalytic amount of piperidine as catalyst. Compound (2) is the key intermediate for the synthesis of several series of new compounds such as ((pyrimidine, tetrazine, piperidine, oxazepine)-2H-coumarin-2-one derivatives by reaction with selected reagents such as urea, cyanoacetamide, cyanoacetohydrazide, orthoaminophenol and 5-aminotriazole.
Synthesis and Characterization of Schiff Base from Aromatic Amine and Aromati...ijtsrd
The synthesis of Schiff base From Aromatic Amine And Aromatic P Nitro benzaldehyde was performed by a novel method of stirring followed by the addition of p nitro benzaldehydeandm nitro aniline 0.02M . Characterization of the synthesized compounds, determination of purity and identity of the compounds using following spectroscopic and chromatographic techniques Solubility, Thin Layer Chromatographic studies, Ultra Violet studied rotational and vibrational studies FT IR studies. The compounds were investigated for their Antimicrobial activity by cup plate method. Compound1 nitro 4 1 imino,4 nitrophenyl benzene was found to be the most active according to pharmacological evaluation exhibited antimicrobial. Ms. Chetana D. Patil | Mr. Digamber N. Bhosale | Ms. Smita P. Bedis "Synthesis and Characterization of Schiff Base from Aromatic Amine and Aromatic P-Nitro Benzaldehyde" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-3 | Issue-5 , August 2019, URL: https://www.ijtsrd.com/papers/ijtsrd26401.pdfPaper URL: https://www.ijtsrd.com/pharmacy/medicinal-chemistry/26401/synthesis-and-characterization-of-schiff-base-from-aromatic-amine-and-aromatic-p-nitro-benzaldehyde/ms-chetana-d-patil
This document summarizes the synthesis of new C-2, C-3 substituted heterocyclic derivatives of L-ascorbic acid and their characterization and evaluation of bacterial activity. Specifically, it describes the multi-step synthesis of Schiff bases and 1,3-oxazepine derivatives from L-ascorbic acid, including protection of hydroxyl groups, esterification, hydrazide formation, Schiff base formation with substituted benzaldehydes, and Diels-Alder reaction with phthalic anhydride to form 1,3-oxazepines. The synthesized compounds were characterized using melting point, FTIR, and 1H NMR spectroscopy and tested for antibacterial activity against gram-positive and
IJERA (International journal of Engineering Research and Applications) is International online, ... peer reviewed journal. For more detail or submit your article, please visit www.ijera.com
The document describes a new synthesis method for bisacodyl, a substituted diphenyl(2-pyridyl)methane derivative that has laxative activity. The key steps involve migrating a 2-pyridacyl group from phenyl pyridine-2-carboxylate to form 4-hydroxyphenyl(2-pyridyl) ketone when reacted with aluminum chloride, then condensing this intermediate with phenol in the presence of phosphoric acid to form the target bisacodyl compound. This new method uses more readily available pyridine-2-carboxylic acid as a starting material compared to existing synthesis routes
An efficient synthesis, characterization and antibacterial activity of novel ...iosrjce
IOSR Journal of Applied Chemistry (IOSR-JAC) is a double blind peer reviewed International Journal that provides rapid publication (within a month) of articles in all areas of applied chemistry and its applications. The journal welcomes publications of high quality papers on theoretical developments and practical applications in Chemical Science. Original research papers, state-of-the-art reviews, and high quality technical notes are invited for publications.
Synthesis and Characterization O-, M- and Para-Toluyl Thiourea Substituted Pa...IOSR Journals
Abstract: Six new derivatives of carbonyl thiourea comprises of o-,m- and p-toluyl at one end of Nitrogen atom and p-methylpyridine or ethyl pyridine at another one end of Nitrogen atom has been synthesized. The compounds are, 2-methyl-N-[(4-methylpyridine-2-yl) carbamothiol] benzamide (I), 3-methyl-N-[(4-methylpyridine-2-yl) carbamothiol] benzamide (II) and 4-N-[(4-methylpyridine-2-yl) carbamothiol] benzamide (III) for Toluyl-MP while 2-methyl-N-[(2-pyridine-2-yl-ethyl) carbamothiol] benzamide (IV), 3- methyl-N-[(2-pyridine-2-yl-ethyl) carbamothiol] benzamide (V) and 4- methyl-N-[(2-pyridine-2-yl-ethyl) carbamothiol] benzamide (VI) for isomer Toluidal-AEP have been successfully synthesized and characterized by elemental analysis, Infrared Spectroscopy analysis (FT-IR), Nuclear Magnetic Resonance Spectroscopy (NMR) and Ultraviolet-visible (UV-vis). All products shown stretching modes of ν(N-H), ν(C=O), ν(C-N), and ν(C=S) around 3276 cm-1, 1671 cm-1, 1315cm-1 and 1148 cm-1 respectively. All products shown two maximum absorption around 262 nm and 290 nm respectively for carbonyl C=O and thione C=S chromophore. Those both values contributed by n -п* transition. 1H nuclear magnetic resonance spectrum showed presence of aromatic, methyl, methine and amide protons except for product III. All products showed presence of carbon thione in 13C nuclear magnetic resonance except for product III. Ionophor interpretation with acetate anion shows color changes by naked eye for compound (I) and (III).
This document describes chemoenzymatic syntheses of segments of scytonemin A and HPA-12. Lipase-catalyzed kinetic resolutions were used to obtain enantiomerically pure secondary alcohols. Both (2R,6S)-13 and (2S,6S)-13 were obtained as precursors for scytonemin A synthesis. For HPA-12, alcohol dehydrogenase reaction of (S)-15 yielded (S)-17, the required precursor. Chemoenzymatic steps produced varying enantiomeric excesses depending on substrate structure and lipase used.
A new and efficient synthesis of 1 (4-subtitued phenyl)-3-(1-(6-(substitued-2...Alexander Decker
This document describes a new efficient method for the synthesis of 1-(4-Subtitued phenyl)-3-(1-(6-(Substitued-2-yl)pyrimidin-4-yl)piperidin-4-yl)ureas. Tert-butyl (1-(6-chloropyrimidin-4-yl)piperidin-4-yl)carbamate is coupled with various arylboronic acids using Suzuki coupling to yield intermediates. These intermediates are then deprotected and coupled with various aryl isocyanates using triethylamine to yield the final urea products in good yields. In total, twelve new 4,6-disubstituted
The document provides information about Schiff bases:
- Schiff bases are organic compounds formed by the condensation of carbonyl compounds with primary amines, first reported in 1864.
- There are several methods for synthesizing Schiff bases, including microwave, reflux, stirring, and grinding methods. Spectroscopic techniques like FT-IR, UV-Vis, and X-ray spectroscopy are used to characterize Schiff bases and their complexes.
- Schiff bases have applications in coordination chemistry and as intermediates in organic synthesis. They also show biological activities like antimicrobial and anticancer properties.
Synthesis and Biological Evaluation of Novel3, 5-Disubstituted 4h-1, 2, 4-Tri...IOSR Journals
A general method was developed for the synthesis of novel unsymmetrical 3, 5-disubstituted 4H-1, 2,
4-triazoles with benzyl group in the 4-ring position (5a-j). A series of novel N-acyl amidrazone derivatives (4a-j)
have been synthesized. The chemical structures of newly synthesis zed compounds were characterized by IR,
H1NMR,C13NMR and mass. The newly synthesized compounds were screened for antimicrobial activity
Polycondensation of Ethylenediaminetetraacetic Acid with SomeTaghreed Al-Noor
Many condensed polymers [A1-A7] were prepared via reaction of (Ethylenediaminetetraacetic acid = EDTA),
with different prepared imide-diamines by modification [ modification of amino acids and antibiotics (B1-
B7)]
Imide-diamines were prepared by chlorination of L-amino acids such as
[ L-Histidine, L-Alanine, L-Valine, L-Glycine and L-Aspargine ] or selected antibiotics such as [Cephallixine
monohydrate and Amoxilline ] with thionyl chloride at 0°C, then reacted with ammonia to obtain imidediamines
[B1-B7] .
The physical properties of all prepared condensed polymers [A1-A7], new prepared diamines [B1-B7] were
studied and characterized by FT -IR spectroscope to certify the structural formulas.
The thermal analysis (TGA, DTA) were studied, and the intrinsic viscosities were measured at 30°C using
Ostwald viscometer.
Synthesis & characterization of saccharine derivativesAlexander Decker
This document describes the synthesis and characterization of 15 saccharine derivatives. Saccharine was reacted with various carbonyl-containing compounds, ketones, aldehydes, esters, and diesters or amide compounds to form new open chain compounds. The synthesized compounds were characterized using techniques such as melting point determination, FT-IR, H-NMR, and elemental analysis. FT-IR showed characteristic absorption bands corresponding to functional groups present. H-NMR indicated peaks corresponding to protons of functional groups. Elemental analysis and melting points supported the proposed structures and purity of the compounds.
This document describes an efficient synthetic route to produce ethyl 2-aryl-4-hydroxy-1,3(2H,4H)-dioxoisoquinoline-4-carboxylates, which are known to inhibit auxin transport in plants and have plant growth regulating properties. The synthesis involves condensing anilines with homophthalic anhydride to form intermediates, which are then modified through various steps including acylation, enolate formation, alcoholysis, and oxygenation to produce the target compounds. Several of the target compounds showed potent auxin transport inhibition and plant growth regulating activity in tests.
Carboxy-terminal Degradation of Peptides using Perfluoroacyl Anhydrides : C-T...Keiji Takamoto
This document describes a new method for determining the carboxy-terminal (C-terminal) amino acid sequence of peptides using perfluoroacyl anhydride vapor. Exposure of peptides to the vapor at -20°C for 0.5-1 hours sequentially degrades the peptide from the C-terminus. Analysis of the truncated peptide fragments by fast-atom-bombardment mass spectrometry allows determination of the C-terminal sequence based on mass differences. The method provides C-terminal sequence information as a complement to the common Edman degradation method for amino-terminal sequencing. The perfluoroacyl anhydride vapor method results in more extensive C-terminal degradation than a previous method using perfluoric acid
Complexation, Spectroscopic, Thermal, Magnetic And Conductimetric Studies On ...IOSR Journals
7-hydroxy-4-methyl-8-(phenylazo) coumarin (L1)and 7-hydroxy-4-methyl-8-(o-carboxyphenylazo) coumarin (L2) have been prepared and characterized by elemental analysis, infrared (IR), proton nuclear magnetic resonance (1H NMR) and Mass spectra. The important infrared (IR) spectral bands corresponding to the active groups in the two ligands and the solid complexes under investigation were studied. Also the important fragments in the ligands and the complexes were done using mass spectra and the main peaks were corresponding to the molecular weights of the ligands and complexes. The solid complexes have been synthesized and studied by elemental and thermal analyses (TG and DTA) as well as by IR, 1H NMR, magnetic measurements, electronic transition, molar conductance, mass spectra and electron spin resonance (ESR) spectra. The proposed steriochemical structures for the investigated metal complexes suggest octahedral geometry with respect to Mn, Co, Ni, Cu and Zn metal ions and all of the formed complexes contain coordinated and hydrated water molecules. All of the prepared solid complexes behave as non-electrolytes in chloroform.
Synthesis And Antibacterial Activity Of 3-[(3-Phenyl-5-Thioxo-1, 5-Dihydro-4h...inventionjournals
A series of 3-[(3-phenyl-5-thioxo-1,5-dihydro-4H-1,2,4-triazol-4-yl)imino]-1,3-dihydro-2Hindole-2-one derivatives were synthesised through the nucleophilic substitution at carbonyl carbon of Isatin. Structure of synthesized compounds were elucidated by using IR, 1H NMR & 13C NMR spectrometry. Synthesised compounds showed significant antibacterial activity against E.coli (ATCC 35218), S.aureus (ATCC 25323), E.faecalis (Clinical isolate), K. Pneumonia, P. aeruginosa (ATCC 27893) using agar well diffusion method.
Synthesis and characterization of resin copolymer derived from cardanol-furfu...ijceronline
International Journal of Computational Engineering Research (IJCER) is dedicated to protecting personal information and will make every reasonable effort to handle collected information appropriately. All information collected, as well as related requests, will be handled as carefully and efficiently as possible in accordance with IJCER standards for integrity and objectivity.
This document describes an inter-laboratory evaluation study conducted to validate the use of the 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay as a standard method for evaluating the antioxidant capacity of food additives. Fourteen laboratories participated in the study. Five analytical samples - four existing food additives (tea extract, grape seed extract, enju extract, and d-α-tocopherol) and Trolox - were evaluated using the DPPH assay. The results showed good repeatability for measuring antioxidant capacity within laboratories, but greater variability between laboratories. However, expressing the results as Trolox equivalent antioxidant capacity reduced inter-laboratory variability, suggesting the DPPH assay could be
Synthesis of new 2 h pyrano[3,2-h]quinolines with potential biological activityAlexander Decker
The document summarizes the synthesis of new 2H-pyrano[3,2-h]quinoline derivatives with potential biological activity. 5-halo-8-hydroxyquinoline-7-carboxaldehyde reacted with diethyl malonate to produce ethyl 6-halo-2-oxo-2H-pyrano[3,2-h]quinoline-3-carboxylates, which underwent further reactions to form derivatives containing pyrane, pyrazole, indole and oxadiazino[5,6-b]indole moieties. The biological screening showed some of the pyrano[3,2-h]quinoline derivatives have excellent antibacterial and ant
This document summarizes the total synthesis of 2,6-dideoxy-2,6-imino-7-O-β-D-glucopyranosyl-D-glycero-L-gulo-heptitol hydrochloride (8), a potent inhibitor of α-glucosidases. The key steps involve homologation and amination of 2,3,4,6-tetra-O-benzyl-D-glucopyranose (1) to form the protected amine 4. An intramolecular cyclization of 4 catalyzed by mercuric acetate formed the piperidine ring. Glycosylation of aglycon 6 with acetob
Synthesis of 3-Substituted Coumarins by the Knoevenagel Condensation Reactionmariam1020
The document summarizes a study on the synthesis of 3-substituted coumarins via the Knoevenagel condensation reaction of various 2-hydroxyaldehydes and malonate esters under solvent-free conditions using silica gel or basic alumina as catalyst. The reaction was carried out using microwave irradiation. Various coumarin products were obtained in moderate to good yields and characterized using techniques such as IR, NMR, and GC-MS. The method provides an improvement over traditional Knoevenagel condensation reactions through the use of solvent-free conditions and microwave activation.
1,4- Addition of copper acetylides to unsaturated ketonesSaibalendu Sarkar
TMSI promoted 1,4-addition of Copper acetylides to unsaturated aldehydes and ketones.This ppt is totally based on a paper published in Journal of American Chemical Society. The ppt is more about the analysis of the paper
International Journal of Pharmaceutical Science Invention (IJPSI) is an international journal intended for professionals and researchers in all fields of Pahrmaceutical Science. IJPSI publishes research articles and reviews within the whole field Pharmacy and Pharmaceutical Science, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
Synthesis Characterization And Antimicrobial Activity Of 6- Oxido-1- ((5 -5- ...IOSR Journals
This document describes the synthesis and characterization of several novel carbamate derivatives and their evaluation for antimicrobial activity. Specifically, it details the multi-step synthesis of cyclopropyl/cyclohexyl/terahydro-2H-pyran-4-yl/tetrahydro-2H-thiopyran-4-yl/perfluorophenyl (6-oxido-1-((5-(5-(pyridin-3-yl)-1H-tetrazol-1-yl)-1,3,4-thiadiazol-2-yl)methyl)-4,8-dihydro-1H-[1,3,2]dioxaphosphepino
This document describes the design, synthesis, and evaluation of benzimidazolo/tetrazolo quinazoline compounds. Specifically, it details the reaction of anthranilic acid with primary amides to form quinazolinones, which were then treated with phosphorus oxychloride and phosphorus pentachloride to form chloroquinazolines. These compounds then reacted with o-phenylenediamine or sodium azide to form the target benzimidazolo or tetrazolo quinazolines. The compounds were evaluated for their antihyperglycemic activity in sucrose-loaded rat models, with the benzimidazolo quinazolines showing better but still low activity
An efficient synthesis, characterization and antibacterial activity of novel ...iosrjce
IOSR Journal of Applied Chemistry (IOSR-JAC) is a double blind peer reviewed International Journal that provides rapid publication (within a month) of articles in all areas of applied chemistry and its applications. The journal welcomes publications of high quality papers on theoretical developments and practical applications in Chemical Science. Original research papers, state-of-the-art reviews, and high quality technical notes are invited for publications.
Synthesis and Characterization O-, M- and Para-Toluyl Thiourea Substituted Pa...IOSR Journals
Abstract: Six new derivatives of carbonyl thiourea comprises of o-,m- and p-toluyl at one end of Nitrogen atom and p-methylpyridine or ethyl pyridine at another one end of Nitrogen atom has been synthesized. The compounds are, 2-methyl-N-[(4-methylpyridine-2-yl) carbamothiol] benzamide (I), 3-methyl-N-[(4-methylpyridine-2-yl) carbamothiol] benzamide (II) and 4-N-[(4-methylpyridine-2-yl) carbamothiol] benzamide (III) for Toluyl-MP while 2-methyl-N-[(2-pyridine-2-yl-ethyl) carbamothiol] benzamide (IV), 3- methyl-N-[(2-pyridine-2-yl-ethyl) carbamothiol] benzamide (V) and 4- methyl-N-[(2-pyridine-2-yl-ethyl) carbamothiol] benzamide (VI) for isomer Toluidal-AEP have been successfully synthesized and characterized by elemental analysis, Infrared Spectroscopy analysis (FT-IR), Nuclear Magnetic Resonance Spectroscopy (NMR) and Ultraviolet-visible (UV-vis). All products shown stretching modes of ν(N-H), ν(C=O), ν(C-N), and ν(C=S) around 3276 cm-1, 1671 cm-1, 1315cm-1 and 1148 cm-1 respectively. All products shown two maximum absorption around 262 nm and 290 nm respectively for carbonyl C=O and thione C=S chromophore. Those both values contributed by n -п* transition. 1H nuclear magnetic resonance spectrum showed presence of aromatic, methyl, methine and amide protons except for product III. All products showed presence of carbon thione in 13C nuclear magnetic resonance except for product III. Ionophor interpretation with acetate anion shows color changes by naked eye for compound (I) and (III).
This document describes chemoenzymatic syntheses of segments of scytonemin A and HPA-12. Lipase-catalyzed kinetic resolutions were used to obtain enantiomerically pure secondary alcohols. Both (2R,6S)-13 and (2S,6S)-13 were obtained as precursors for scytonemin A synthesis. For HPA-12, alcohol dehydrogenase reaction of (S)-15 yielded (S)-17, the required precursor. Chemoenzymatic steps produced varying enantiomeric excesses depending on substrate structure and lipase used.
A new and efficient synthesis of 1 (4-subtitued phenyl)-3-(1-(6-(substitued-2...Alexander Decker
This document describes a new efficient method for the synthesis of 1-(4-Subtitued phenyl)-3-(1-(6-(Substitued-2-yl)pyrimidin-4-yl)piperidin-4-yl)ureas. Tert-butyl (1-(6-chloropyrimidin-4-yl)piperidin-4-yl)carbamate is coupled with various arylboronic acids using Suzuki coupling to yield intermediates. These intermediates are then deprotected and coupled with various aryl isocyanates using triethylamine to yield the final urea products in good yields. In total, twelve new 4,6-disubstituted
The document provides information about Schiff bases:
- Schiff bases are organic compounds formed by the condensation of carbonyl compounds with primary amines, first reported in 1864.
- There are several methods for synthesizing Schiff bases, including microwave, reflux, stirring, and grinding methods. Spectroscopic techniques like FT-IR, UV-Vis, and X-ray spectroscopy are used to characterize Schiff bases and their complexes.
- Schiff bases have applications in coordination chemistry and as intermediates in organic synthesis. They also show biological activities like antimicrobial and anticancer properties.
Synthesis and Biological Evaluation of Novel3, 5-Disubstituted 4h-1, 2, 4-Tri...IOSR Journals
A general method was developed for the synthesis of novel unsymmetrical 3, 5-disubstituted 4H-1, 2,
4-triazoles with benzyl group in the 4-ring position (5a-j). A series of novel N-acyl amidrazone derivatives (4a-j)
have been synthesized. The chemical structures of newly synthesis zed compounds were characterized by IR,
H1NMR,C13NMR and mass. The newly synthesized compounds were screened for antimicrobial activity
Polycondensation of Ethylenediaminetetraacetic Acid with SomeTaghreed Al-Noor
Many condensed polymers [A1-A7] were prepared via reaction of (Ethylenediaminetetraacetic acid = EDTA),
with different prepared imide-diamines by modification [ modification of amino acids and antibiotics (B1-
B7)]
Imide-diamines were prepared by chlorination of L-amino acids such as
[ L-Histidine, L-Alanine, L-Valine, L-Glycine and L-Aspargine ] or selected antibiotics such as [Cephallixine
monohydrate and Amoxilline ] with thionyl chloride at 0°C, then reacted with ammonia to obtain imidediamines
[B1-B7] .
The physical properties of all prepared condensed polymers [A1-A7], new prepared diamines [B1-B7] were
studied and characterized by FT -IR spectroscope to certify the structural formulas.
The thermal analysis (TGA, DTA) were studied, and the intrinsic viscosities were measured at 30°C using
Ostwald viscometer.
Synthesis & characterization of saccharine derivativesAlexander Decker
This document describes the synthesis and characterization of 15 saccharine derivatives. Saccharine was reacted with various carbonyl-containing compounds, ketones, aldehydes, esters, and diesters or amide compounds to form new open chain compounds. The synthesized compounds were characterized using techniques such as melting point determination, FT-IR, H-NMR, and elemental analysis. FT-IR showed characteristic absorption bands corresponding to functional groups present. H-NMR indicated peaks corresponding to protons of functional groups. Elemental analysis and melting points supported the proposed structures and purity of the compounds.
This document describes an efficient synthetic route to produce ethyl 2-aryl-4-hydroxy-1,3(2H,4H)-dioxoisoquinoline-4-carboxylates, which are known to inhibit auxin transport in plants and have plant growth regulating properties. The synthesis involves condensing anilines with homophthalic anhydride to form intermediates, which are then modified through various steps including acylation, enolate formation, alcoholysis, and oxygenation to produce the target compounds. Several of the target compounds showed potent auxin transport inhibition and plant growth regulating activity in tests.
Carboxy-terminal Degradation of Peptides using Perfluoroacyl Anhydrides : C-T...Keiji Takamoto
This document describes a new method for determining the carboxy-terminal (C-terminal) amino acid sequence of peptides using perfluoroacyl anhydride vapor. Exposure of peptides to the vapor at -20°C for 0.5-1 hours sequentially degrades the peptide from the C-terminus. Analysis of the truncated peptide fragments by fast-atom-bombardment mass spectrometry allows determination of the C-terminal sequence based on mass differences. The method provides C-terminal sequence information as a complement to the common Edman degradation method for amino-terminal sequencing. The perfluoroacyl anhydride vapor method results in more extensive C-terminal degradation than a previous method using perfluoric acid
Complexation, Spectroscopic, Thermal, Magnetic And Conductimetric Studies On ...IOSR Journals
7-hydroxy-4-methyl-8-(phenylazo) coumarin (L1)and 7-hydroxy-4-methyl-8-(o-carboxyphenylazo) coumarin (L2) have been prepared and characterized by elemental analysis, infrared (IR), proton nuclear magnetic resonance (1H NMR) and Mass spectra. The important infrared (IR) spectral bands corresponding to the active groups in the two ligands and the solid complexes under investigation were studied. Also the important fragments in the ligands and the complexes were done using mass spectra and the main peaks were corresponding to the molecular weights of the ligands and complexes. The solid complexes have been synthesized and studied by elemental and thermal analyses (TG and DTA) as well as by IR, 1H NMR, magnetic measurements, electronic transition, molar conductance, mass spectra and electron spin resonance (ESR) spectra. The proposed steriochemical structures for the investigated metal complexes suggest octahedral geometry with respect to Mn, Co, Ni, Cu and Zn metal ions and all of the formed complexes contain coordinated and hydrated water molecules. All of the prepared solid complexes behave as non-electrolytes in chloroform.
Synthesis And Antibacterial Activity Of 3-[(3-Phenyl-5-Thioxo-1, 5-Dihydro-4h...inventionjournals
A series of 3-[(3-phenyl-5-thioxo-1,5-dihydro-4H-1,2,4-triazol-4-yl)imino]-1,3-dihydro-2Hindole-2-one derivatives were synthesised through the nucleophilic substitution at carbonyl carbon of Isatin. Structure of synthesized compounds were elucidated by using IR, 1H NMR & 13C NMR spectrometry. Synthesised compounds showed significant antibacterial activity against E.coli (ATCC 35218), S.aureus (ATCC 25323), E.faecalis (Clinical isolate), K. Pneumonia, P. aeruginosa (ATCC 27893) using agar well diffusion method.
Synthesis and characterization of resin copolymer derived from cardanol-furfu...ijceronline
International Journal of Computational Engineering Research (IJCER) is dedicated to protecting personal information and will make every reasonable effort to handle collected information appropriately. All information collected, as well as related requests, will be handled as carefully and efficiently as possible in accordance with IJCER standards for integrity and objectivity.
This document describes an inter-laboratory evaluation study conducted to validate the use of the 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay as a standard method for evaluating the antioxidant capacity of food additives. Fourteen laboratories participated in the study. Five analytical samples - four existing food additives (tea extract, grape seed extract, enju extract, and d-α-tocopherol) and Trolox - were evaluated using the DPPH assay. The results showed good repeatability for measuring antioxidant capacity within laboratories, but greater variability between laboratories. However, expressing the results as Trolox equivalent antioxidant capacity reduced inter-laboratory variability, suggesting the DPPH assay could be
Synthesis of new 2 h pyrano[3,2-h]quinolines with potential biological activityAlexander Decker
The document summarizes the synthesis of new 2H-pyrano[3,2-h]quinoline derivatives with potential biological activity. 5-halo-8-hydroxyquinoline-7-carboxaldehyde reacted with diethyl malonate to produce ethyl 6-halo-2-oxo-2H-pyrano[3,2-h]quinoline-3-carboxylates, which underwent further reactions to form derivatives containing pyrane, pyrazole, indole and oxadiazino[5,6-b]indole moieties. The biological screening showed some of the pyrano[3,2-h]quinoline derivatives have excellent antibacterial and ant
This document summarizes the total synthesis of 2,6-dideoxy-2,6-imino-7-O-β-D-glucopyranosyl-D-glycero-L-gulo-heptitol hydrochloride (8), a potent inhibitor of α-glucosidases. The key steps involve homologation and amination of 2,3,4,6-tetra-O-benzyl-D-glucopyranose (1) to form the protected amine 4. An intramolecular cyclization of 4 catalyzed by mercuric acetate formed the piperidine ring. Glycosylation of aglycon 6 with acetob
Synthesis of 3-Substituted Coumarins by the Knoevenagel Condensation Reactionmariam1020
The document summarizes a study on the synthesis of 3-substituted coumarins via the Knoevenagel condensation reaction of various 2-hydroxyaldehydes and malonate esters under solvent-free conditions using silica gel or basic alumina as catalyst. The reaction was carried out using microwave irradiation. Various coumarin products were obtained in moderate to good yields and characterized using techniques such as IR, NMR, and GC-MS. The method provides an improvement over traditional Knoevenagel condensation reactions through the use of solvent-free conditions and microwave activation.
1,4- Addition of copper acetylides to unsaturated ketonesSaibalendu Sarkar
TMSI promoted 1,4-addition of Copper acetylides to unsaturated aldehydes and ketones.This ppt is totally based on a paper published in Journal of American Chemical Society. The ppt is more about the analysis of the paper
International Journal of Pharmaceutical Science Invention (IJPSI) is an international journal intended for professionals and researchers in all fields of Pahrmaceutical Science. IJPSI publishes research articles and reviews within the whole field Pharmacy and Pharmaceutical Science, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
Synthesis Characterization And Antimicrobial Activity Of 6- Oxido-1- ((5 -5- ...IOSR Journals
This document describes the synthesis and characterization of several novel carbamate derivatives and their evaluation for antimicrobial activity. Specifically, it details the multi-step synthesis of cyclopropyl/cyclohexyl/terahydro-2H-pyran-4-yl/tetrahydro-2H-thiopyran-4-yl/perfluorophenyl (6-oxido-1-((5-(5-(pyridin-3-yl)-1H-tetrazol-1-yl)-1,3,4-thiadiazol-2-yl)methyl)-4,8-dihydro-1H-[1,3,2]dioxaphosphepino
This document describes the design, synthesis, and evaluation of benzimidazolo/tetrazolo quinazoline compounds. Specifically, it details the reaction of anthranilic acid with primary amides to form quinazolinones, which were then treated with phosphorus oxychloride and phosphorus pentachloride to form chloroquinazolines. These compounds then reacted with o-phenylenediamine or sodium azide to form the target benzimidazolo or tetrazolo quinazolines. The compounds were evaluated for their antihyperglycemic activity in sucrose-loaded rat models, with the benzimidazolo quinazolines showing better but still low activity
Synthesis And Characterization of Novel Processable Poly (EtherAzomethine)S C...inventionjournals
The novel dialdehyde 1,1-bis[4-(4-benzaldehyde oxy) phenyl] cyclopentane (III) (BBPC) was synthesized starting from cyclopentanone and phenol to give 1, 1-Bis (4-hydroxy phenyl) cyclopentane (II); followed by reaction with p- fluorobenzaldehyde in N, N-dimethyl formamide (DMAc), containing anhydrous potassium carbonate. New series of poly (ether – azomethine)s were synthesized from (BBPC) with different diamines such as 4, 4’- diamino diphenyl ether (ODA),4,4’-diaminodiphenyl methane(MDA),4-aminophenyl sulfone(SDA), p-phenylene diamines, etc. in DMAc with 5 wt% LiCl by solution polycondensation technique. Inherent viscosities of these polymers were in the range 0.19 to 0.42 dL/g indicating formation of moderate molecular weights. These polymers exhibited good solubility in various polar aprotic solvents such as Nmethylpyrrolidone (NMP), N, N-dimethylacetamide (DMAc) and N,N-dimethyl formamide (DMF), etc. X-Ray diffraction pattern of polymers showed that introduction of cardo cyclopentylidene moiety containing ether linkage would disrupt the chain regularity and packing, leading to amorphous nature. Thermal analysis by TGA showed excellent thermal stability of polymers. The structure- property correlation among these polyazomethines were studied; in view of their potential applications as high performance polymers.
Synthesis, Characterization and invitro Anti- inflammatory activity of 1, 3, ...SriramNagarajan19
Oxadiazole derivatives have played a vital part in the development of heterocyclic compounds. In this present work, a series of 5-(2-aminophenyl)-1,3,4-oxadiazole-2(3H)-thione derivatives (1-10) have been synthesized by Mannich reaction. The reaction progress of the synthesized compounds was checked by TLC. The structures of the newly synthesized compounds were confirmed by IR and 1H NMR spectral data. The in-vitro anti-inflammatory activity of 1, 3, 4-oxadiazole compounds (1-10) was assessed by HRBC Membrane Stabilization Method. Among the newly synthesized 1,3,4-oxadiazole derivatives, compounds OFP, OAP, OBNP, OPBNP, ORP, OUP, OPClBP, OFD, OAD and OBND possessed highly significant anti-inflammatory activity at a dose of 1000µg/ml when compared with standard, Diclofenac potassium.
International Journal of Engineering Research and Applications (IJERA) is an open access online peer reviewed international journal that publishes research and review articles in the fields of Computer Science, Neural Networks, Electrical Engineering, Software Engineering, Information Technology, Mechanical Engineering, Chemical Engineering, Plastic Engineering, Food Technology, Textile Engineering, Nano Technology & science, Power Electronics, Electronics & Communication Engineering, Computational mathematics, Image processing, Civil Engineering, Structural Engineering, Environmental Engineering, VLSI Testing & Low Power VLSI Design etc.
The document describes the synthesis and characterization of 9-anilinoacridine derivatives substituted with oxazine moieties to evaluate their antioxidant and anticancer activities. A series of 9-anilinoacridines were synthesized by reacting 1-[4-(acridin-9-ylamino)phenyl]ethanone with various aldehydes using Claisen-Schmidt condensation. The structures of the synthesized compounds were confirmed using spectroscopic techniques like IR, NMR, mass spectrometry. The compounds were evaluated for their antioxidant activity by hydrogen peroxide and superoxide radical scavenging assays. Their anticancer potential was studied against Dalton's lymphoma ascites cell line using trypan blue dye exclusion and
Oxidation of 7-Methyl Sulfanyl-5-Oxo-5H-Benzothiazolo-[3, 2-A]-Pyrimidine-6-...inventionjournals
International Journal of Engineering and Science Invention (IJESI) is an international journal intended for professionals and researchers in all fields of computer science and electronics. IJESI publishes research articles and reviews within the whole field Engineering Science and Technology, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
A new Schiff base 4-chlorophenyl)methanimine
(6R,7R)-3-methyl-8-oxo-7-(2-phenylpropanamido)-5-thia-1-
azabicyclo[4.2.0]oct-2-ene-2-carboxylate= (HL)= C23H20
ClN3O4S) has been synthesized from β-lactam antibiotic
(cephalexin mono hydrate(CephH)=(C16H19N3O5S.H2O) and 4-
chlorobenzaldehyde . Figure(1) Metal mixed ligand complexes
of the Schiff base were prepared from chloride salt of
Fe(II),Co(II),Ni(II),Cu(II),Zn(II) and Cd (II), in 50% (v/v)
ethanol –water medium (SacH ) .in aqueous ethanol(1:1)
containing and Saccharin(C7H5NO3S) = sodium hydroxide.
Several physical tools in particular; IR, CHN, 1H NMR, 13C
NMR for ligand and melting point molar conductance, magnetic
moment. and determination the percentage of the metal in the
complexes by flame(AAS). The ligands and there metal
complexes were screened for their antimicrobial activity against
four bacteria (gram + ve) and (gram -ve) {Escherichia coli,
Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus}.
The proposed structure of the complexes using program, Chem
office 3D(2006). The general formula have been given for the
prepared mixed ligand complexes Na2[M(Sac)3(L)], M(II) = Fe
(II), Co(II) , Ni(II), Cu (II), Zn(II) , and Cd(II).
HL= C29H24 ClN3O4S, L= C29H23 ClN3O4S -.
Synthesis and Characterization of cyclohexylidene containing novel cardo pol...inventionjournals
International Journal of Engineering and Science Invention (IJESI) is an international journal intended for professionals and researchers in all fields of computer science and electronics. IJESI publishes research articles and reviews within the whole field Engineering Science and Technology, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
This document describes the synthesis of a new heterocyclic indigo dye called 2-(1, 3- dihydro- 3 - oxo- 2H - pyridylpyrr- 2- ylidene)-1, 2-dihydro- 3H- pyridylpyrrol- 3-one. It was synthesized in two steps: first, an aromatic glycine intermediate was synthesized from 2-aminopyridine, monochloroacetic acid, and sodium hydroxide. Second, this glycine intermediate was fused with sodamide, sodium hydroxide, and potassium hydroxide, then oxidized using acidified ferric chloride to yield the final dye compound. Spectral analysis
This document summarizes the synthesis and spectral analysis of a novel benzyl derivative of ciprofloxacin (Cip-D) and its copper(II) and cobalt(II) complexes. Cip-D was synthesized by reacting ciprofloxacin with benzyl chloride in the presence of triethylamine to introduce an amide group. Spectral analysis using 1H NMR, IR, and mass spectroscopy confirmed the structure of Cip-D and indicated bonding between the metal ions and Cip-D in the complexes. Analysis showed shifts in peaks for the complexes, indicating coordination between the metal ions and Cip-D. The Cip-D and its Cu(II) and Co(II)
This document describes the synthesis of novel spirooxindole derivatives via a three-component 1,3-dipolar cycloaddition reaction. Various spirooxindole-spiropiperidinone-pyrrolidine and spirooxindole-spiropiperidinone-pyrrolizine derivatives were synthesized in good yields from isatin, sarcosine or L-proline, and Knoevenagel adducts under optimized reaction conditions. The antimicrobial activities of the synthesized compounds were evaluated, with some compounds exhibiting excellent activity against bacteria and fungi, comparable or superior to standard antimicrobial drugs.
Syntheses and Characterizations of Some New N-alkyl, Isoxazole and Dioxazole ...IJAEMSJORNAL
N-alkyl and cycloadducts derivatives of 5-Chloroisatin were synthesized in good to excellent yields. The method evidences a selective N-alkylation when using 1,2-bis (2-chloroethoxy) ethane as efficient spacer at room temperature on the 5-Chloroisatin moiety. A general method for the 1,3-dipolar cycloaddition of 4-Chlorobenzaldoxime to alkynes provides a useful alternative route to get newisoxazole et dioxazole derivatives.
This document describes a facile synthetic route for producing the alpha-glucosidase inhibitor 2,6-dideoxy-2,6-imino-7-O-beta-D-glucopyranosyl-D-glycero-L-gulo-heptitol (1) in 26% overall yield from nojirimycin bisulfite adduct (2). Key steps include: (1) appending a nitrile group to (2) to form an intermediate (3), (2) hydrolyzing (3) to the carboxylic acid (6), and (3) condensing (6) with a protected glucose donor to form the glucoside (9), which
An Efficient Synthetic Approach Towards 4-Cyano-3-(Methylthio)-5-Oxo-2H-Pyraz...inventionjournals
ABSTRACT: Synthesis of novel heterocyclic 4-cyano -3-(methylthio)-5-oxo-2H-pyrazole-1(5H)- carbothioamide (3) was prepared by condensing ethyl-2-cyano-3,3-bis (methylthio)acrylate (1) with thiosemicarbazide (2) in DMF and catalytic amount of potassium carbonate. Compound (3) has methylthio group at third position, which is replaced by different nucleophiles such as substituted anilines| phenols| hetryl amines| compounds containing active methylene group to afford 3-substituted derivatives of compound (3). All the newly synthesized compounds were screened for their antimicrobial activity.
The document summarizes research on the synthesis and characterization of mixed ligand metal complexes derived from ampicillin drug and 4-(dimethylamino)benzaldehyde. A Schiff base ligand was prepared via the condensation of these compounds. Metal complexes were synthesized using Fe(II), Co(II), Ni(II), Cu(II), and Zn(II) with the ligand and nicotinamide. The complexes were characterized using various analytical techniques and showed octahedral geometry. The complexes and ligand were screened for antimicrobial activity against bacteria. The complexes demonstrated higher antimicrobial activity than the free ligand.
New Schiff base ligand (E)-6-(2-(4-
(dimethylamino)benzylideneamino)-2-phenylacetamido)-3,3-
dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic
acid = (HL) Figure(1) was prepared via condensation of
Ampicillin and 4(dimethylamino)benzaldehyde in methanol
.Polydentate mixed ligand complexes were obtained from 1:1:2
molar ratio reactions with metal ions and HL, 2NA on reaction
with MCl2 .nH2O salt yields complexes corresponding to the
formulas [M(L)(NA)2Cl] ,where M =
Fe(II),Co(II),Ni(II),Cu(II),and Zn(II) and NA=nicotinamide.
The 1H-NMR, FT-IR, UV-Vis and elemental analysis
were used for the characterization of the ligand. The complexes
were structurally studied through AAS, FT-IR, UV-Vis,
chloride contents, conductance, and magnetic susceptibility
measurements. All complexes are non-electrolytes in DMSO
solution. Octahedral geometries have been suggested for each
of the complexes. The Schiff base ligands function as
tridentates and the deprotonated enolic form is preferred for
coordination. In order to evaluate the effect of the bactericidal
activity, these synthesized complexes, in comparison to the un
complexed Schiff base has been screened against bacterial
species, Staphy
A series of novel 5-[2-(4-fluorobenzyl)-6-aryl-imidazo[2,1-b][1,3,4]thiadiazol-5-ylmethylene] thiazolidine-2,4-dione derivatives (4a-d) were synthesized. These final compounds (4a-d) were synthesized by Knoevenagel condensation of 2-(4-fluorobenzyl)-6-arylimidazo[2,1-b][1,3,4]thiadiazole-5-carbaldehydes (3a-d) with thiazolidine-2,4-dione. All the newly synthesized compounds were screened for their invivo hypoglycemic and hypolipidemic activity in male Wister rats. The Structures of all the newly synthesized compounds were established by analytical and spectral data.
Facial and Simple Synthesis of Some New (Pyrazole and Triazole) Coumarin Deri...IOSRJAC
2-oxo-2H-coumarin-3-carbohydrazide (2) which prepared from the reaction of ethyl-2-oxo-2Hcoumarin-3-carboxylate (1) with hydrazine hydrate in ethanol containing a catalytic amount of piperidine mixture consider a good and available starting intermediate for synthesis of series of functionalized coumarins. So, compound (2) was utilized as a key for the synthesis of some new (pyrazole, triazole)-2H- coumarin-2-one derivatives by the reaction with some selected reagents.
Similar to Synthesis, Characterization and Study of Antioxidant Activities of Some New Pyrazoline Derivatives Containing Isatin Moiety (20)
Exploratory study on the use of crushed cockle shell as partial sand replacem...IJRES Journal
The increasing demand for natural river sand supply for the use in construction industry along
with the issue of environmental problem posed by the dumping of cockle shell, a by-product from cockle
business have initiated research towards producing a more environmental friendly concrete. This research
explores the potential use of cockle shell as partial sand replacement in concrete production. Cockle shell used
in this experimental work were crushed to smaller size almost similar to sand before mixed in concrete. A total
of six concrete mixtures were prepared with varying the percentages of cockle shell viz. 0%, 5%, 10%, 15%,
20% and 25%. All the specimens were subjected to continuous water curing. The compressive strength test was
conducted at 28 days in accordance to BS EN 12390. Finding shows that integration of suitable content of
crushed cockle shell of 10% as partial sand replacement able to enhance the compressive strength of concrete.
Adopting crushed cockle shell as partial sand replacement in concrete would reduce natural river sand
consumption as well as reducing the amount of cockle shell disposed as waste.
Congenital Malaria: Correlation of Umbilical Cord Plasmodium falciparum Paras...IJRES Journal
The vertical (trans-placental) transmission of the parasite Plasmodium falciparum from
pregnant mother to fetus during gestational period was investigated in a clinical research involving 43 full term
pregnant women in selected Hospitals in Jimeta Yola, Adamawa State Nigeria. During the observational study,
parasitemia was determined by light microscopic examination of umbilical and maternal peripheral blood film
for the presence of the trophozoites of Plasmodium falciparum. Correlational analysis was then carried on the
result obtained at p<0.05.><0.05) was established between maternal peripheral blood and umbilical cord
blood parasitemia with Pearson’s correlation coefficient of 0.762. Thus, in a malaria endemic area like Yola,
Adamawa State, Nigeria, with a stable transmission of parasite, there is a high probability of vertical
transmission of Plasmodium falciparum parasite from mother to fetus during gestation that can be followed by
the presentation of the symptoms of malaria by the newborn and other malaria related complications. Families
are advised to consistently sleep under appropriately treated insecticide mosquito net to avoid mosquito bite and
subsequent infestation.
Review: Nonlinear Techniques for Analysis of Heart Rate VariabilityIJRES Journal
Heart rate variability (HRV) is a measure of the balance between sympathetic mediators of heart
rate that is the effect of epinephrine and norepinephrine released from sympathetic nerve fibres acting on the
sino-atrial and atrio-ventricular nodes which increase the rate of cardiac contraction and facilitate conduction at
the atrio-ventricular node and parasympathetic mediators of heart rate that is the influence of acetylcholine
released by the parasympathetic nerve fibres acting on the sino-atrial and atrio-ventricular nodes leading to a
decrease in the heart rate and a slowing of conduction at the atrio-ventricular node. Sympathetic mediators
appear to exert their influence over longer time periods and are reflected in the low frequency power(LFP) of
the HRV spectrum (between 0.04Hz and 0.15 Hz).Vagal mediators exert their influence more quickly on the
heart and principally affect the high frequency power (HFP) of the HRV spectrum (between 0.15Hz and 0.4
Hz). Thus at any point in time the LFP:HFP ratio is a proxy for the sympatho- vagal balance. Thus HRV is a
valuable tool to investigate the sympathetic and parasympathetic function of the autonomic nervous system.
Study of HRV enhance our understanding of physiological phenomenon, the actions of medications and disease
mechanisms but large scale prospective studies are needed to determine the sensitivity, specificity and predictive
values of heart rate variability regarding death or morbidity in cardiac and non-cardiac patients. This paper
presents the linear and nonlinear to analysis the HRV.
Dynamic Modeling for Gas Phase Propylene Copolymerization in a Fluidized Bed ...IJRES Journal
The document presents a dynamic two-phase model for a fluidized bed reactor used to produce polypropylene. The model divides the reactor into an emulsion phase and bubble phase, with reaction assumed to occur in both phases. Simulation results show the temperature profile is lower than previous single-phase models due to considering both phases. Approximately 13% of the produced polymer comes from the bubble phase, demonstrating the importance of accounting for both phases.
Study and evaluation for different types of Sudanese crude oil propertiesIJRES Journal
Sudanese crude oil is regarded as one of the sweet types of crude in the world, Sulphur containing
compounds are un desirable in petroleum because they de activate the catalyst during the refining processes and
are the main source of acid rains and environmental pollution.(Mark Cullen 2001),Since it contains considerable
amount of salts and acids, it negatively impact the production facilities and transportation lines with corrosive
materials. However it suffers other problems in flow properties represented by the high viscosity and high
percentage of wax. Samples were collected after the initial and final treatment at CPF, and tested for
physical and chemical properties.wax content is in the range 23-31 weight % while asphalting content is about
0.1 weight% . Resin content is 13-7 weight % and deposits are 0.01 weight%. The carbon number distribution in
the crude is in the range 7-35 carbon atoms. The pour point vary between 39°C-42°C and the boiling point is in
the range 70 °C - 533 °C.
A Short Report on Different Wavelets and Their StructuresIJRES Journal
This article consists of basics of wavelet analysis required for understanding of and use of wavelet
theory. In this article we briefly discuss about HAAR wavelet transform their space and structures.
A Case Study on Academic Services Application Using Agile Methodology for Mob...IJRES Journal
Recently, Mobile Cloud Computing reveals many modern development areas in the Information
Technology industry. Several software engineering frameworks and methodologies have been developed to
provide solutions for deploying cloud computing resources on mobile application development. Agile
methodology is one of the most commonly used methodologies in the field. This paper presents the MCCAS a
Web and Mobile application that provide feature for the Palestinian higher education/academic institutions. An
Agile methodology was used in the development of the MCCAS but in parallel with emphasis on Cloud
computing resources deployment. Also many related issues is discussed such as how software engineering
modern methodologies (advances) influenced the development process.
Wear Analysis on Cylindrical Cam with Flexible RodIJRES Journal
Firstly, the kinetic equation of spatial cylindrical cam with flexible rod has been established. Then, an
accurate cylindrical cam mechanism model has been established based on the spatial modeling software
Solidworks. The dynamic effect of flexible rod on mechanical system was studied in detail based on the
mechanical system dynamics analytical software Adams, and Archard wear model is used to predict the wear of
the cam. We used Ansys to create finite element model of the cam link, extracted the first five order mode to
export into Adams. The simulation results show that the dynamic characteristics of spatial cylindrical cam
mechanical system with flexible rod is closed to ideal mechanism. During the cam rotate one cycle, the collision
in the linkage with a clearance occurs in some special location, others still keep a continuous contact, and the
prediction of wear loss is smaller than rigid body.
DDOS Attacks-A Stealthy Way of Implementation and DetectionIJRES Journal
Cloud Computing is a new paradigm provides various host service [paas, saas, Iaas over the internet.
According to a self-service,on-demand and pay as you use business model,the customers will obtain the cloud
resources and services.It is a virtual shared service.Cloud Computing has three basic abstraction layers System
layer(Virtual Machine abstraction of a server),Platform layer(A virtualized operating system, database and
webserver of a server and Application layer(It includes Web Applications).Denial of Service attack is an attempt
to make a machine or network resource unavailable to the intended user. In DOS a user or organization is
deprived of the services of a resource they would normally expect to have.A Successful DOS attack is a highly
noticeable event impacting the entire online user base.DOS attack is found by First Mathematical Metrical
Method (Rate Controlling,Timing Window,Worst Case and Pattern Matching)DOS attack not only affect the
Quality of the service and also affect the performance of the server. DDOS attacks are launched from Botnet-A
large Cluster of Connected device(cellphone,pc or router) infected with malware that allow remote control by an
attacker. Intruder using SIPDAS in DDOS to perform attack.SIPDAS attack strategies are detected using Heap
Space Monitoring Algorithm.
An improved fading Kalman filter in the application of BDS dynamic positioningIJRES Journal
Aiming at the poor dynamic performance and low navigation precision of traditional fading
Kalman filter in BDS dynamic positioning, an improved fading Kalman filter based on fading factor vector is
proposed. The fading factor is extended to a fading factor vector, and each element of the vector corresponds to
each state component. Based on the difference between the actual observed quantity and the predicted one, the
value of the vector is changed automatically. The memory length of different channel is changed in real time
according to the dynamic property of the corresponding state component. The actual observation data of BDS is
used to test the algorithm. The experimental results show that compared with the traditional fading Kalman filter
and the method of the third references, the positioning precision of the algorithm is improved by 46.3% and
23.6% respectively.
Positioning Error Analysis and Compensation of Differential Precision WorkbenchIJRES Journal
The document analyzes positioning errors in differential precision workbenches and proposes a compensation method. It discusses sources of error in workbench transmission systems and guides. Through theoretical analysis and experimentation, it is shown that positioning errors increase with travel distance due to factors like guideway errors. A method is developed to sample positioning at multiple points, compare values to identify errors, and implement reverse error correction through motion control cards. This allows positioning accuracy better than 15 micrometers over 150mm of travel to be achieved. The compensation method can improve precision for a range of machine tool designs.
Status of Heavy metal pollution in Mithi river: Then and NowIJRES Journal
The Mithi River runs through the heart of suburban Mumbai. Its path of flow has been severely
damaged due to industrialization and urbanization. The quality of water has been deteriorating ever since. The
Municipal and industrial effluents are discharged in unchecked amounts. The municipal discharge comprises
untreated domestic and sewage wastes whereas the industries are majorly discharge chemicals and other toxic
effluents which are responsible in increasing the metal load of the river. In the current study, the water is
analysed for heavy metals- Copper, Cadmium, Chromium, Lead and Nickel. It also includes a brief
understanding on the fluctuations that have occurred in the heavy metal pollution, through the compilation of
studies carried out in the area previously.
The Low-Temperature Radiant Floor Heating System Design and Experimental Stud...IJRES Journal
In order to analyze the temperature distribution of the low-temperature radiant floor heating system
that uses the condensing wall-hung boiler as the heat source, the heating system is designed according to a typical
house facing south in Shanghai. The experiments are carried out to study the effects of the supply water
temperature on the thermal comfort of the system. Eventually, the supply water temperature that makes people in
the room feel more comfortable is obtained. The result shows that in the condition of that the outside temperature
is 8~15℃ and the relative humidity is 30~70%RH, the temperature distribution in the room is from high to low
when the height is from bottom to top. The floor surface temperature is highest, but its uniformity is very poor.
When the heating system reaches the steady state, the air temperature of the room is uniform. When the supply
water temperature is 63℃ The room is relatively comfortable at the above experimental condition.
Experimental study on critical closing pressure of mudstone fractured reservoirsIJRES Journal
This study examines the critical closing pressure of fractures in mudstone reservoir cores from the Daqing oilfield in China. Laboratory experiments subjected fractured and unfractured mudstone cores to increasing external pressures while measuring permeability. The critical closing pressure is defined as the pressure when fractured core permeability matches unfractured permeability, indicating fracture closure. Results show fractured cores have higher permeability than unfractured cores due to fractures. Permeability generally decreases exponentially with increasing pressure. By calculating sensitivity equations relating permeability and production pressure difference, the study estimates critical closing pressures under reservoir conditions are lower than values from external pressure experiments. The study provides guidance but notes limitations in fully simulating complex in-situ stress conditions.
Correlation Analysis of Tool Wear and Cutting Sound SignalIJRES Journal
With the classic signal analysis and processing method, the cutting of the audio signal in time
domain and frequency domain analysis. We reached the following conclusions: in the time domain analysis,
cutting audio signals mean and the variance associated with tool wear state change occurred did not change
significantly, and tool wear is not high degree of correlation, and the mean-square value of the audio signal
changes in the size and tool wear the state has a good relationship.
Reduce Resources for Privacy in Mobile Cloud Computing Using Blowfish and DSA...IJRES Journal
Mobile cloud computing in light of the increasing popularity among users of mobile smart
technology which is the next indispensable that enables users to take advantage of the storage cloud computing
services. However, mobile cloud computing, the migration of information on the cloud is reliable their privacy
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processor, Memory and storage. In this paper, we propose a solution to the problem of privacy with saving and
reducing resources power energy, processor and Memory. This is done through data encryption in the mobile
cloud computing by symmetric algorithm and sent to the private cloud and then the data is encrypted again and
sent to the public cloud through Asymmetric algorithm. The experimental results showed after a comparison
between encryption algorithms less time and less time to decryption are as follows: Blowfish algorithm for
symmetric and the DSA algorithm for Asymmetric. The analysis results showed a significant improvement in
reducing the resources in the period of time and power energy consumption and processor.
Resistance of Dryland Rice to Stem Borer (Scirpophaga incertulas Wlk.) Using ...IJRES Journal
Rice stem borer is one of the important pests that attack plants so as to reduce production. One way
to control pests is to use organic fertilizers that make the plant stronger and healthier. This study was conducted
to determine the effects of organic fertilizers with various doses without the use of pesticides in controlling stem
borer, Scirpophaga incertulas. Methods using split-split plot design which consists of two levels of the whole
plot factor (solid and liquid organic fertilizers), two levels of the subplot factor (conventional and industry,
Tiens and Mitraflora), and four levels of the sub-subplot factor of conventional and industry (5, 10, 15, 20
tonnes/ha), and one level of the sub-subplot factor of Tiens and Mitraflora (each 2 ml/l). Based on the results
Statistical analysis there were no significant differences among treatments and this shows that the use of organic
fertilizers that only a dose of 5 tonnes/ha is sufficient available nutrients that make plants more robust and
resistant to control stem borer, besides that can reduce production costs and friendly to the environment when
compared with using inorganic fertilizers.
A novel high-precision curvature-compensated CMOS bandgap reference without u...IJRES Journal
A novel high-precision curvature-compensated bandgap reference (BGR) without using op-amp
is presented in this paper. It is based on second-order curvature correction principle, which is a weighted sum of
two voltage curves which have opposite curvature characteristic. One voltage curve is achieved by first-order
curvature-compensated bandgap reference (FCBGR) without using op-amp and the other found by using W
function is achieved by utilizing a positive temperature coefficient (TC) exponential current and a linear
negative TC current to flow a linear resistor. The exponential current is gained by using anegative TC voltage to
control a MOSFET in sub-threshold region. In the temperature ranging from -40℃ to 125℃, experimental
results implemented with SMIC 0.18μm CMOS process demonstrate that the presented BGR can achieve a TC
as low as 2.2 ppm/℃ and power-supply rejection ratio(PSRR)is -69 dB without any filtering capacitor at 2.0 V.
While the range of the supply voltage is from 1.7 to 3.0 V, the output voltage line regulation is about1 mV/ V
and the maximum TC is 3.4 ppm/℃.
Structural aspect on carbon dioxide capture in nanotubesIJRES Journal
In this work we reported the carbon dioxide adsorption (CO2) in six different nanostructures in order
to investigate the capturing capacity of the materials at nanoscale. Here we have considered the three different
nanotubes including zinc oxide nanotube (ZnONT), silicon carbide nanotube (SiCNT) and single walled carbon
nanotube (SWCNT). Three different chiralities such as zigzag (9,0), armchair (5,5) and chiral (6,4) having
approximately same diameter are analyzed. The adsorption binding energy values under various cases are
estimated with density functional theory (DFT). We observed CO2 molecule chemisorbed on ZnONT and
SiCNT’s whereas the physisorption is predominant in CNT. To investigate the structural aspect, the tubes with
defects are studied and compared with defect free tubes. We have also analyzed the electrical properties of tubes
from HOMO, LUMO energies. Our results reveal the defected structure enhance the CO2 capture and is
predicted to be a potential candidate for environmental applications.
Thesummaryabout fuzzy control parameters selected based on brake driver inten...IJRES Journal
In this paper, the brake driving intention identification parameters based on the fuzzy control are
summarized and analyzed, the necessary parameters based on the fuzzy control of the brake driving intention
recognition are found out, and I pointed out the commonly corrupt parameters, and through the relevant
parameters , I establish the corresponding driving intention model.
Mending Clothing to Support Sustainable Fashion_CIMaR 2024.pdfSelcen Ozturkcan
Ozturkcan, S., Berndt, A., & Angelakis, A. (2024). Mending clothing to support sustainable fashion. Presented at the 31st Annual Conference by the Consortium for International Marketing Research (CIMaR), 10-13 Jun 2024, University of Gävle, Sweden.
PPT on Direct Seeded Rice presented at the three-day 'Training and Validation Workshop on Modules of Climate Smart Agriculture (CSA) Technologies in South Asia' workshop on April 22, 2024.
Authoring a personal GPT for your research and practice: How we created the Q...Leonel Morgado
Thematic analysis in qualitative research is a time-consuming and systematic task, typically done using teams. Team members must ground their activities on common understandings of the major concepts underlying the thematic analysis, and define criteria for its development. However, conceptual misunderstandings, equivocations, and lack of adherence to criteria are challenges to the quality and speed of this process. Given the distributed and uncertain nature of this process, we wondered if the tasks in thematic analysis could be supported by readily available artificial intelligence chatbots. Our early efforts point to potential benefits: not just saving time in the coding process but better adherence to criteria and grounding, by increasing triangulation between humans and artificial intelligence. This tutorial will provide a description and demonstration of the process we followed, as two academic researchers, to develop a custom ChatGPT to assist with qualitative coding in the thematic data analysis process of immersive learning accounts in a survey of the academic literature: QUAL-E Immersive Learning Thematic Analysis Helper. In the hands-on time, participants will try out QUAL-E and develop their ideas for their own qualitative coding ChatGPT. Participants that have the paid ChatGPT Plus subscription can create a draft of their assistants. The organizers will provide course materials and slide deck that participants will be able to utilize to continue development of their custom GPT. The paid subscription to ChatGPT Plus is not required to participate in this workshop, just for trying out personal GPTs during it.
The debris of the ‘last major merger’ is dynamically youngSérgio Sacani
The Milky Way’s (MW) inner stellar halo contains an [Fe/H]-rich component with highly eccentric orbits, often referred to as the
‘last major merger.’ Hypotheses for the origin of this component include Gaia-Sausage/Enceladus (GSE), where the progenitor
collided with the MW proto-disc 8–11 Gyr ago, and the Virgo Radial Merger (VRM), where the progenitor collided with the
MW disc within the last 3 Gyr. These two scenarios make different predictions about observable structure in local phase space,
because the morphology of debris depends on how long it has had to phase mix. The recently identified phase-space folds in Gaia
DR3 have positive caustic velocities, making them fundamentally different than the phase-mixed chevrons found in simulations
at late times. Roughly 20 per cent of the stars in the prograde local stellar halo are associated with the observed caustics. Based
on a simple phase-mixing model, the observed number of caustics are consistent with a merger that occurred 1–2 Gyr ago.
We also compare the observed phase-space distribution to FIRE-2 Latte simulations of GSE-like mergers, using a quantitative
measurement of phase mixing (2D causticality). The observed local phase-space distribution best matches the simulated data
1–2 Gyr after collision, and certainly not later than 3 Gyr. This is further evidence that the progenitor of the ‘last major merger’
did not collide with the MW proto-disc at early times, as is thought for the GSE, but instead collided with the MW disc within
the last few Gyr, consistent with the body of work surrounding the VRM.
Current Ms word generated power point presentation covers major details about the micronuclei test. It's significance and assays to conduct it. It is used to detect the micronuclei formation inside the cells of nearly every multicellular organism. It's formation takes place during chromosomal sepration at metaphase.
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ESR spectroscopy in liquid food and beverages.pptxPRIYANKA PATEL
With increasing population, people need to rely on packaged food stuffs. Packaging of food materials requires the preservation of food. There are various methods for the treatment of food to preserve them and irradiation treatment of food is one of them. It is the most common and the most harmless method for the food preservation as it does not alter the necessary micronutrients of food materials. Although irradiated food doesn’t cause any harm to the human health but still the quality assessment of food is required to provide consumers with necessary information about the food. ESR spectroscopy is the most sophisticated way to investigate the quality of the food and the free radicals induced during the processing of the food. ESR spin trapping technique is useful for the detection of highly unstable radicals in the food. The antioxidant capability of liquid food and beverages in mainly performed by spin trapping technique.
Describing and Interpreting an Immersive Learning Case with the Immersion Cub...Leonel Morgado
Current descriptions of immersive learning cases are often difficult or impossible to compare. This is due to a myriad of different options on what details to include, which aspects are relevant, and on the descriptive approaches employed. Also, these aspects often combine very specific details with more general guidelines or indicate intents and rationales without clarifying their implementation. In this paper we provide a method to describe immersive learning cases that is structured to enable comparisons, yet flexible enough to allow researchers and practitioners to decide which aspects to include. This method leverages a taxonomy that classifies educational aspects at three levels (uses, practices, and strategies) and then utilizes two frameworks, the Immersive Learning Brain and the Immersion Cube, to enable a structured description and interpretation of immersive learning cases. The method is then demonstrated on a published immersive learning case on training for wind turbine maintenance using virtual reality. Applying the method results in a structured artifact, the Immersive Learning Case Sheet, that tags the case with its proximal uses, practices, and strategies, and refines the free text case description to ensure that matching details are included. This contribution is thus a case description method in support of future comparative research of immersive learning cases. We then discuss how the resulting description and interpretation can be leveraged to change immersion learning cases, by enriching them (considering low-effort changes or additions) or innovating (exploring more challenging avenues of transformation). The method holds significant promise to support better-grounded research in immersive learning.
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Synthesis, Characterization and Study of Antioxidant Activities of Some New Pyrazoline Derivatives Containing Isatin Moiety
1. International Journal of Research in Engineering and Science (IJRES)
ISSN (Online): 2320-9364, ISSN (Print): 2320-9356
www.ijres.org Volume 1 Issue 7 ǁNov. 2013 ǁPP.08-13
www.ijres.org 8 | Page
Synthesis, Characterization and Study of Antioxidant Activities of
Some New Pyrazoline Derivatives Containing Isatin Moiety
Kiran Dasary*, Asha Lavania, Manju Yadav and Anita V K Anand
*Department of chemistry, School of chemical sciences, St. John’s College, Agra, 282002 INDIA
ABSTRACT : A series of substituted pyrazoline derivatives 5(a-c) have been synthesized by the reaction of
substituted chalcones 4(a-c) with isatinhydrazide. The starting materials, chalcones were prepared by clasien
schimidt condensation of appropriate 1-hydroxy-2-acetonaphthone with substituted aldehydes in the presence of
sodium hydroxide and in poly ethylene glycol (PEG-400). The structures of the synthesized compounds were
confirmed by IR, 1HNMR & Mass spectral data. The synthesized compounds were screened for Antioxidant
Activity by DPPH method.
Keywords: Pyrrole, Chalcones, Pyrazolines, Isatin, PEG (400), Antioxidant Activity
I. INTRODUCTION
Pyrazolines are well known and important nitrogen containing five-membered heterocyclic compounds
and various methods have been worked out for their synthesis. Numerous pyrazoline derivatives have been
found to possess considerable biological activities, which stimulated the research activity in this field. They
have found to possess anti-fungal[1],anti-depressant [2-7 ],anti-convulsant [8], anti-inflammatory [9-12], anti-
bacterial [13-14], anti-cancer[15-18], anti-pyretic[19], anti-neoplastic activities [20-21], anti-viral [22], anti-
amoebic [23-24], acaricidal agro chemical fungicides or insecticides [25], anti-cholinergic [26-27], antidiabetic
[28], anti-HIV [29-32], anti-malarial [33], anesthetic [34], anaxiolytic [35], antiparasitic[ 36], anti-allergic[37],
anti-microbial [38-40], anti-tuberculosis[41-44], tyrosinase inhibitor [45], blue photo luminescence and electro
luminescence [46], food and chemical toxicology [47], herbicidal [48-50], hypoglycaemic [51], hypertensive
[52], immunosuppressive[53], anti-tumor[54]. Moreover, many selectively chloro-substituted organic
compounds show peculiar pharmacological and agrochemical properties.
Based on the above biological activities exhibited by the pyrazoline compounds, we report here, the
synthesis and biological evaluation of some new pyrazoline derivatives. Chalcones (4a-c) were prepared from
substituted aldehydes and ketones, in presence of alkali NaOH and poly ethylene glycol (PEG-400) as solvent
medium. The later compounds (4a-c) were converted into the title compounds (5a-c) by reacting with
isatinhydrazide in glacial acetic acid medium.
Isatinhydrazides are important classes of nitrogen containing heterocycles and they constitute useful
intermediates in organic synthesis [55-57]. They have been reported for their applications in dyes and have also
been used as building blocks for the synthesis of organic semiconductors. More interestingly studies have
discovered that these compounds exhibit diverse medical functions such as antioxidant properties. [58-59].
II. MATERIALS AND METHODS
2-hydroxy-1-aceto naphthone, all aromatic aldehydes, hydrazine hydrate were purchased from Sigma
Aldrich. PEG used was of Thomas baker. Ethanol and other chemicals of A.R. grade were used as received.
General procedure for the Synthesis 3-Pyrrol-1-yl-1,3-dihydro-indol-2-one (1): 1H-Indole-2,3-dione (Isatin)
( 0.5mmol), 4-hydroxy -L-proline (0.5 mmol) and InCl3 (10 mol%) were stirred in 2 ml of EtOH at 80 ℃ and the
reaction progress was monitored by TLC. After the completion of the reaction, the solvent was evaporated and
the crude product was purified by flash chromatography (ethyl acetate∶ petroleum ether.
General procedure for the Synthesis of (2-Oxo-3-pyrrol-1-yl-2, 3-dihydro-indol-1-yl)-acetic acid ethyl
ester (2): 3-Pyrrol-1-yl-1, 3-dihydro-indol-2-one (0.5mmol), ethylchloroacetate (0.05mmol) and potassium
carbonate (0.10mmol) in dry acetone was refluxed for 20 h. The reaction mixture was poured onto crushed ice,
and the solid was then filtered, washed with water and recrystallised from methanol.
General procedure for the synthesis of (2-Oxo-3-pyrrol-1-yl-2,3-dihydro-indol-1-yl)-acetic acid hydrazide
(3): (2-Oxo-3-pyrrol-1-yl-2,3-dihydro-indol-1-yl)-acetic acid ethyl ester (10 mmol) and N2H4.H2O (25 mmol) in
10 cm3
ethanol was heated under reflux for 4h.The excess of ethanol was removed under reduced pressure and
the resulting precipitate was filtered off, washed with ethanol, and recrystallized from ethanol
2. Synthesis, Characterization and Study of Antioxidant Activities of Some New Pyrazoline Derivatives
www.ijres.org 9 | Page
General procedure for the synthesis of chalcones (4a-c): A solution of 1-hydroxy-2-acetonaphthone (1mmol)
in poly ethylene glycol (PEG-400) (2ml) and substituted aromatic aldehyde (1.1.mmol) was added. To this
mixture aqueous sodium hydroxide (40%, 10 ml) was poured gradually while stirring a soid mass was obtained.
The mixture was kept at room temperature for 1-5 hrs. Then poured into crushed ice and acidified with HCl
(30%). The solid separated was filtered and recrystallized from ethanol.
General procedure for the Synthesis of Pyrazoline Derivatives (5a-c): The solution of appropriate Chalcone
(0.01mol) and (2-Oxo-3-pyrrol-1-yl-2, 3-dihydro-indol-1-yl)-acetic acid hydrazide (0.02 mol) in ethanolic
sodium hydroxide 20 ml was refluxed for 4 hour. The product was poured into ice water and the crude product
which was separated out was filtered and crystallised from proper solvent.
Physical
measurements
and analytical
data: The entire compounds obtained were purified by column chromatography using silica-gel (100-200
mesh). Hexane/ethyl acetate was used as an eluent. 1
H and 13
C NMR were recorded on a Bruker AV-400
spectrometer operating at 400, 100 MHz respectively, using tetramethylsilane (TMS) in the solvent of CDCl3 as
the internal standard (1
H NMR: TMS at 0.00 ppm, CDCl3 at 7.26 ppm; 13
C NMR: CDCl3 at 77.0 ppm) or were
recorded using tetramethylsilane (TMS) in the solvent of DMSO-d6 as the internal standard (1
H NMR: TMS at
0.00 ppm, DMSO at 2.50 ppm; 13
C NMR: DMSO at 39.5 ppm. The coupling constants J are given in Hz. IR
spectra were recorded on FT/IR-5300. Elemental analysis was performed on Thermo Finningan FLASH EA
1112 CHN analyzer. IR spectra (In KBr pellets) were recorded on a Shimadzu FT-IR 5300 spectrophotometer.
Reactions were monitored by TLC silica coated plates obtained from Merck. Commercially available reagents
and solvents were used without further purification and were purchased. Melting points were measured in open
capillary tubes and are uncorrected.
InCl3
ROH, Reflux N
H
N
O
N
H
O
O
1
N
H
HO
COOH
+
Scheme 1
N
N
O
O
O
N
N
O
NH
O
H2N
Reflux/EtoH
N2H4.H2O
2 3
700
C
Scheme 2
N
H
N
O
1
Ethylchloroacetate
Dry Acetone/Reflux
OOH
O H
R1
OOH
R1
4a-c
(Scheme 3)
Where 4a = R1= -Cl, 4b = R1 = -NO2, 4c = R1= H
PEG(400)
NaOH
Where 5a = R1= -Cl, 5b = R1 = -NO2, 5c = R1= H
OOH
R1
4a-c
OH R1
N
N
N
O
Reflux/Ethanol
N
70-800
C
Hydrazide (3)
5a-c
(Scheme 4)
O
3. Synthesis, Characterization and Study of Antioxidant Activities of Some New Pyrazoline Derivatives
www.ijres.org 10 | Page
III. RESULTS AND DISCUSSION
1-(1-Hydroxy-naphthalen-2-yl)-3-phenyl-propenone (4a-c) were prepared by carrying out the reactions
of 2-hydroxy-1-aceto naphthone with 4-chloro benzaldehyde, 4-nitro benzaldehyde, benzaldehyde and ethanol
using aqueous sodium hydroxide and (PEG-400) as a catalyst. Synthesis of chalcone is a single step method.
The synthesized chalcones were condensed with Isatin hydrazide to form pyrazoline derivatives (5a-c). All the
synthesized compounds have been reported their elemental analysis for the percentage of carbon, hydrogen,
oxygen and nitrogen was found to be experimentally equivalent to the calculated values.
The data obtained of the synthesized compounds –
(1) 3-Pyrrol-1-yl-1, 3-dihydro-indol-2-one: White amorphous powder: %; m.p. 140°C. Anal.: Calcd. for
C12H10N2O: Calcd, C,72.71;H,5.08; N,14.13;(%)Found: C,72.43; H ,5.19; N,14.22; (%)IR (KBr,
nmax, cm-1): , 3194, 1717, 1618, 1466, 1
H NMR (CDCl3, 400 MHz): δ 5.46 (s, 1H), 6.17 (t, 2H, J
= 2.21 Hz), 6.63 (t, 2H, J = 2.21 Hz), 6.85-7.09 (m, 2H), 7.20-7.33 (m, 2H), 9.5 (brs, 1H) MS
m/z 198 (M+).
(2) (2-Oxo-3-pyrrol-1-yl-2,3-dihydro-indol-1-yl)-acetic acid ethyl ester: brick red solid: yield: 95 %; m.p.
230˚C; Anal.Calcd. for C16H16N2O3: C, 67.59; H, 5.67 (%); Found: C, 67.65; H, 5.69 (%) IR (KBr, nmax, cm-
1):-1650 (C=O), 1585, 1560 (C=C), 1
H NMR (CDCl3, 400 MHz): δ 7.79-7.78 (m, 1H), 7.51 (d, J = 3.8 Hz, 1H),
7.08-7.07 (m, 1H), 4.34 (q, J = 5.8 Hz, 2H), 1.36 (t, J = 5.4 Hz, 3H). 13
C NMR (CDCl3, 100 MHz): δ 162.2,
134.0, 133.2, 132.1, 127.8, 127.6, 61.1, 14.3; MS m/z 285 (M+).
(3) (2-Oxo-3-pyrrol-1-yl-2, 3-dihydro-indol-1-yl)-acetic acid hydrazide: white power: yield: 90 %; m.p.1860
C;
Anal.: calcd. (%) for C14H14N4O2: C, 62.21; H, 5.22; N, 20.73; Found (%): C, 62.25; H, 5.29; N, 20.75; IR (KBr,
nmax, cm-1):- 3433, 3337(NH), 1669(C=O), 1612(C=N); MS m/z 270 (M+).
(4a) 3-(2-Chloro-phenyl)-1-(1-hydroxy-naphthalen-2-yl)-propenone: light creamy solid: Yield: 91 %; m.p.
130˚C; Anal.Calcd. for C20H16O3Cl: C, 79.47; H, 6.03 (%); Found: C, 78.67; H, 5.61 IR (KBr, nmax, cm-1):-
3100 (OH), 1722 (CO), 1645 (CH=CH), 855 (C-Cl); 1H NMR (400 MHz, CDCl3) d9.44 (1H, d, J = 9Hz, C-8c-
H), 7.95 (1H, d, J = 16Hz, C-7-H), 7.75 (1H, d, J = 16 Hz, C-8-H), 7.60-7.70 (2H, m, C-4c and 5c-H), 7.55-7.65
(2H, d, C-3 and C-5), 7.39-7.56 (4H, m, C-2 and C-6, C-6c and 7c-H), 7.20 (1H, d, J= 9 Hz, C-3c-H). MS m/z
308 (M+).
(4b) 1-(1-Hydroxy-naphthalen-2-yl)-3-(4-nitro-phenyl)-propenone: brown solid: Yield: 90%; m.p. 165˚C;
Anal.Calcd. for C19H13NO4: C, 71.46; H, 4.10 (%); Found: C, 71.83; H, 4.12 (%);IR (KBr, nmax, cm-1):- 3100
(OH), 1721 (C=]O), 1640 (CH=CH), 1345 (C-N); 1H NMR (400 MHz, CDCl3) d 13.5 (1H, s, C-2c-OH), 9.47
(1H, d, J = 9Hz, C-8c-H), 7.98 (1H, d, J = 16Hz, C-7-H), 7.77 (1H, d, J = 16 Hz, C-8-H), 7.71 (2H, s, C-2 and
4-H), 7.62- 7.68 (2H, m, C-4c and 5c-H), 7.28-7.55 (4H, m, C-5,6 and 6c, 7c-H ), 7.17 (1H, d, J = 9 Hz, C-3c-
H); MS m/z 318 (M+).
(4c) 1-(1-Hydroxy-naphthalen-2-yl)-3-phenyl-propenone: light green solid: Yield: 90%; 80; m.p. 160˚C;
Anal.Calcd. for C19H14O2: C, 83.19; H, 5.14(%); Found: C, 85.19; H, 5.16 (%); IR (KBr, nmax, cm-1):-3446
(OH),, 1614, 1743; 1
H NMR (CDCl3, 400 MHz): δ 7.79-7.78 (m, 1H), 7.51 (d, J = 3.8 Hz, 1H), 7.08-7.07 (m,
1H), 4.34 (q, J = 5.8 Hz, 2H), 1.36 (t, J = 5.4 Hz, 3H). 13
C NMR (CDCl3, 100 MHz): δ 162.2, 134.0, 133.2,
132.1, 127.8, 127.6, 61.1, 14.3; MS m/z 385 (M+).
(5a)1-[5-(4-Chloro-phenyl)-3-(1-hydroxy-naphthalen-2-yl)-4,5-dihydro-pyrazol-1-ylmethyl]-3-pyrrol-1-yl-1,3-
dihydro-indol-2-one: light brown solid: Yield: 80%; mp 190˚C; Anal.Calcd. for C32H25ClN4O2: C, 72.11; H,
4.73; N, 10.51(%); Found: C, 72.13; H, 4.75; N, 10.53 (%); IR (KBr, nmax, cm-1):- 3110 (OH), 3042 (CH),
1594 (C=N), 1722 (C=O), 855 (C-Cl); MS m/z 533 (M+).
(5b) 1-[3-(1-Hydroxy-naphthalen-2-yl)-5-(4-nitro-phenyl)-4,5-dihydro-pyrazol-1-ylmethyl]-3-pyrrol-1-yl-1,3-
dihydro-indol-2-one: yellowish red solid: Yield: 75%; mp 140˚C; Anal.Calcd. for C32H25N5O4: C, 70.71; H,
4.64; N, 12.88 (%); Found C, 70.73; H, 4.67; N, 14.88 (%);IR (KBr, cm-1): 3110 (OH), 3042 (CH), 1676
(C=O), 1593 (C=N), 1542 (-NO2) MS m/z 543 (M+).
(5c) 1-[3-(1-Hydroxy-naphthalen-2-yl)-5-phenyl-4,5-dihydro-pyrazol-1-ylmethyl]-3-pyrrol-1-yl-1,3-dihydro-
indol-2-one: dark green solid: Yield: 90 %; mp 135˚C; Anal.Calcd. for C32H26N4O2: C, 77.09; H, 5.26; N,
11.24(%); Found C, 77.10; H, 5.28; N, 11.26 (%);IR (KBr, nmax, cm-1) 3120 (OH), 3042 (CH), 1682 (C=O),
1593 (C=N); MS m/z 497 (M+).
Screeing for Antioxidant activity by DPPH Method
DPPH assay: (2, 2-diphenyl-1-picrylhydrazyl):
DPPH is a common abbreviation for an organic chemical compound 2,2-diphenyl-1-picrylhydrazyl. It
is a crystalline powder composed of stable free-radical molecules. DPPH has two major applications, both in
laboratory research: one is a monitor of chemical reactions involving radicals, most notably it is a common
antioxidant assay.
.
4. Synthesis, Characterization and Study of Antioxidant Activities of Some New Pyrazoline Derivatives
www.ijres.org 11 | Page
Control-Test
Control
Principle:
The scavenging reaction between DPPH and antioxidant (H-A) can be written as:
(DPPH) + (H-A) → DPPH-H + (A)
(Purple) (Yellow)
Antioxidants react with DPPH., which is a stable free radical and is reduced to the DPPHH
and as consequence the absorbance’s decreased from the DPPH radical to the DPPH-H form. The degree
of discoloration indicates the scavenging potential of the antioxidant compounds or extracts in terms of
hydrogen donating ability.
Materials required:
1. Methanolic solution of DPPH (0.1 mM): 39.4 mg of DPPH was dissolved in one liter of
analytical grade methanol.
2. Test sample
Antioxidant activity (using DPPH Method)
0.1mM solution of DPPH in methanol was prepared and 1.0 ml of this solution was added to 3.0 ml of
extract solution in methanol at different concentration (1-16 µg/ml). Thirty minutes later, the absorbance
was measured at 517 nm. A blank was prepared without adding sample. Lower the absorbance of the reaction
mixture indicates higher free radical scavenging activity (expressed as % inhibition) . The capability to
scavenge the DPPH radical was calculated using the following equation:
DPPH Scavenged (%) = X 100
Control is the absorbance of the methanol in DPPH alone.
Test means the absorbance in the presence of sample.
Antioxidant activity of the different successive compounds mentioned as graphs below.
We have synthesized the above mentioned compound in the laboratory. All the compounds showed the
antioxidant activity and which compound have the pyrrole ring group (5c) showed the more active molecule
comparatively in all other compound as we observed.
Where 1 = 3-Pyrrol-1-yl-1, 3-dihydro-indol-2-one
5. Synthesis, Characterization and Study of Antioxidant Activities of Some New Pyrazoline Derivatives
www.ijres.org 12 | Page
2 = 2-Oxo-3-pyrrol-1-yl-2, 3-dihydro-indol-1-yl)-acetic acid ethyl ester
3 = (2-Oxo-3-pyrrol-1-yl-2, 3-dihydro-indol-1-yl)-acetic acid hydrazide
4a = 3-(2-Chloro-phenyl)-1-(1-hydroxy-naphthalen-2-yl)-propenone
4b = 1-(1-Hydroxy-naphthalen-2-yl)-3-(4-nitro-phenyl)-propenone
4c = 1-(1-Hydroxy-naphthalen-2-yl)-3-phenyl-propenone
5a = 1-[5-(4-Chloro-phenyl)-3-(1-hydroxy-naphthalen-2-yl)-4,5-dihydro-pyrazol-1- .
ylmethyl]-3-pyrrol-1-yl-1,3-dihydro-indol-2-one
5b = 1-[3-(1-Hydroxy-naphthalen-2-yl)-5-(4-nitro-phenyl)-4,5-dihydro-pyrazol-1-ylmethyl]-3-
pyrrol-1-yl-1,3-dihydro-indol-2-one
5c = 1-[3-(1-Hydroxy-naphthalen-2-yl)-5-phenyl-4,5-dihydro-pyrazol-1-ylmethyl]-3-pyrrol-1-yl-1,3-
dihydro-indol-2-one
IV. APPLICATIONS
This is an environmentally benign procedure and reduces the total reaction time and good to excellent
yields of chalcones, pyrrole and pyrazoline derivatives.
V. CONCLUSIONS
In summary, we have synthesized a new series of pyrazoline derivatives containing isatin moiety by the
treatment of 1-(1-Hydroxy-naphthalen-2-yl)-3-phenyl-propenone or substituted chalones with substituted
hydrazides respectively, in ethanol under reflux condition. The synthesis following compounds using PEG (400)
as a catalyst results enhancement in the rate of reaction. The proposed method for the synthesis reduces the total
reaction time and good to excellent yields, also allows easy separation of the product.
VI. ACKNOWLEDGEMENTS
We are thankful to Department of Chemistry, School of Chemical Sciences, St. John’s College, Agra
for providing laboratory facilities and Hyderabad Central University (HCU), Hyderabad, for spectral analysis
and evolution of biological activity.
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