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 Antifungal Evaluation of Some New 1,3,5-Tris...BRNSS Publication Hub
Objective: The objective of the paper was to design, synthesis, and characterization of new 1,3,5-trisubstituted-2-pyrazolines derivative and evaluate for antifungal activity. Materials and Methods: The 1,3,5-tri-substituted-2-pyrazolines derivatives have been synthesized by the reaction of chalcone derivatives with succinic hydrazide in the environment of pyridine. Total 20 compounds have been synthesized and characterized by the IR, 1H NMR, and mass spectral analysis. Antifungal activity of the compounds carried out on four fungal strains, that is, Saccharomyces cerevisiae, Aspergillus niger, Candida albicans, and Rhizopus oryzae in two different concentrations, that is, 50 and 100 μg/ml by agar-diffusion method using cup-plate method and Ketoconazole was used as standard antifungal drug. Results and Discussion: In accordance with the data from antifungal activity, all the synthesized 1,3,5-trisubstituted pyrazole derivatives (ME1-ME8, CL1-CL8, and BR1-BR4) have shown mild to best activity against tested organisms. The data of antifungal activity against the fungal strains (S. cerevisiae, A. niger, C. albicans, and R. oryzae) suggested the order of activity of compounds: BR-3 > BR-2 > BR-1 > CL-4 > BR-4 > CL-3 > CL-2 > ME-3> ME-2 > CL-5 > CL-6 > ME-4 > ME-5 > ME-6 > ME-7 > CL-7 > CL-8 > ME-8 > CL-1 > ME-1. The presence of electronegative group (Br, Cl, F, and NO2) either at third and fifth position of 1,3,5-pyrazoline ring is required for the potent antifungal activity. The presence of electronegative group (Br, Cl) at third and fifth position may necessary for the best activity against bacterial and fungal strains but the addition of F, NO2 has shown the moderate activity but in case of -CH3 and -OCH3 substitution may diminish the activity. The series BR-1 to BR-4 is most active compound of the synthesized compounds. Conclusion: The 1,3,5-trisubstituted pyrazole derivatives has been successfully synthesized and antifungal activity of the compounds denotes that the series BR-1 to BR-4 is most active compound of the all twenty synthesized compounds. The addition of electronegative group (Br, Cl) at third and fifth position in pyrazole ring may necessary for the activity against fungal strains.
The document describes the synthesis and antimicrobial screening of some pyrazolyl heterocycles. Specifically, it details the synthesis of compounds 3, 4, 5, and 6 through various reactions between 1-phenyl-3-(2-pyridyl)-1H-pyrazole-4-carboxaldehyde and acetophenone derivatives. Compound 3 undergo oxidative cyclization to form compounds 4 and 5. Compound 3 also undergoes condensation with hydrazine to form compound 6. The structures of compounds 3, 4, 5, and 6 were characterized using spectral methods. These compounds were then tested for antimicrobial activity against various bacteria and fungi, with some compounds showing moderate to good activity.
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
All manuscripts are subject to rapid peer review. Those of high quality (not previously published and not under consideration for publication in another journal) will be published without delay.
Design, synthesis, characterization and biological evaluation of 3- (4-(7-chl...iosrjce
Novel thiazolidinone derivatives TQ-VI(1-10) were designed, synthesized and screened for
antimicrobial activity. Synthesis of 3-(4-(7-chloro-2-(4-chlorophenyl) 4-oxo-quinazolin-3(4H)-yl) phenyl) -
2-arylthiazolidin-4-one TQ-VI(1-10) have been achieved from the starting material 2-amino-4-chlorobenzoic
acid TQ-I on cyclization with p-chlorobenzoyl chloride TQ-II to yield 7-chloro-2-(4-chlorophenyl)-4H-3,1-
benzoxazin-4-one,TQ-III, which on treatment with p-phenylindiamine gave 3-(4-aminophenyl)-7-chloro-2-(4-
chlorophenyl)quinazolin-4(3H)-one, TQ-IV in good yield. Then, TQ-IV on reaction with substituted aromatic
aldehydes converted to TQ-V(1-10), which on cyclization with thioglycolic acid gave TQ-VI (1-10). All the
synthesized compounds have been characterized on the basis of IR,
1
H-NMR and mass spectral data. The
compounds containing 4-OH, 4-OCH3 and 3,4,5-(OCH3)3 showed good activity. The title compounds were
screened for qualitative (zone of inhibition) and quantitative antimicrobial activity (MIC) by agar cup plate
method and serial dilution technique, respectively. Among the synthesized compounds in the series, the
compound TQVI4 and TQVI5 were found to exhibit significant antifungal activity at lower concentration of
31.25 µg/ml, against A.niger. The compound TQVI5 and TQVI4 showed zone of inhibition of 17mm and 15mm
against A.niger and C.albicans respectively which is comparable to that of standard drug. The rest of the
analogues in the series displayed weak to moderate antimicrobial activity when compared to the standard
positive controls Ampicillin and Amphotericin B.
This document describes the synthesis and characterization of new substituted 1,3,5-triazine compounds containing 1,2,4-triazole and substituted urea/thiourea. The compounds were synthesized in three steps and characterized using techniques such as IR, 1H NMR and elemental analysis. Some of the synthesized compounds (1c, 1e, 1g) showed excellent antimicrobial activity against test microorganisms. The document provides experimental details on the synthesis of the compounds and evaluates their potential as antimicrobial agents.
1. The document describes the synthesis and characterization of new substituted 1,3,5-triazine compounds containing 1,2,4-triazole and substituted urea/thiourea groups.
2. These compounds were synthesized in a stepwise manner and characterized using techniques like IR, NMR and elemental analysis.
3. The antimicrobial activity of the synthesized compounds was evaluated against various microorganisms, with some compounds like 1c, 1e and 1g showing excellent activity.
This document describes the synthesis of 17 new 1,2,4-triazole derivatives and evaluates their antimicrobial and anticancer activities. The compounds showed the most potent antimicrobial activity against the fungus Aspergillus niger. Compound 14 was the most active. Compound 7 exhibited appreciable anticancer activity against colon cancer cells. Quantitative structure-activity relationship analysis identified topological and electronic properties important for the compounds' antimicrobial effects.
Synthesis, characterization and biological activities of novel 2-mercaptobenz...ijperSS
ABSTRACT
A new series of Benzoxazol-2-ylthio-N-(4-substituted) acetohydrazide derivatives (IVa-IVk), were obtained by synthesising new Schiff’s bases derived from benzoxolyl-2-mercaptoaceto hydrazide derivatives by treating with various aryl/hetero aryl aldehydes. Their chemical structures have been confirmed by 1H-NMR, 13C-NMR, FT-IR and ESI-MS spectral data. The synthesised derivatives (IVa-IVk) were screened for their in vitro antimicrobial activities by agar diffusion method. Among the synthesized compounds IVb, IVe, and IVk shown strong antibacterial activity and the compounds IVb, IVe and IVf exhibited strong antifungal activity.
Key words: Benzoxazole, aryl/hetero aryl aldehydes, schiff’s bases, antibacterial activity, antifungal activity.
Synthesis, Characterization, and Antifungal Evaluation of Some New 1,3,5-Tris...BRNSS Publication Hub
Objective: The objective of the paper was to design, synthesis, and characterization of new 1,3,5-trisubstituted-2-pyrazolines derivative and evaluate for antifungal activity. Materials and Methods: The 1,3,5-tri-substituted-2-pyrazolines derivatives have been synthesized by the reaction of chalcone derivatives with succinic hydrazide in the environment of pyridine. Total 20 compounds have been synthesized and characterized by the IR, 1H NMR, and mass spectral analysis. Antifungal activity of the compounds carried out on four fungal strains, that is, Saccharomyces cerevisiae, Aspergillus niger, Candida albicans, and Rhizopus oryzae in two different concentrations, that is, 50 and 100 μg/ml by agar-diffusion method using cup-plate method and Ketoconazole was used as standard antifungal drug. Results and Discussion: In accordance with the data from antifungal activity, all the synthesized 1,3,5-trisubstituted pyrazole derivatives (ME1-ME8, CL1-CL8, and BR1-BR4) have shown mild to best activity against tested organisms. The data of antifungal activity against the fungal strains (S. cerevisiae, A. niger, C. albicans, and R. oryzae) suggested the order of activity of compounds: BR-3 > BR-2 > BR-1 > CL-4 > BR-4 > CL-3 > CL-2 > ME-3> ME-2 > CL-5 > CL-6 > ME-4 > ME-5 > ME-6 > ME-7 > CL-7 > CL-8 > ME-8 > CL-1 > ME-1. The presence of electronegative group (Br, Cl, F, and NO2) either at third and fifth position of 1,3,5-pyrazoline ring is required for the potent antifungal activity. The presence of electronegative group (Br, Cl) at third and fifth position may necessary for the best activity against bacterial and fungal strains but the addition of F, NO2 has shown the moderate activity but in case of -CH3 and -OCH3 substitution may diminish the activity. The series BR-1 to BR-4 is most active compound of the synthesized compounds. Conclusion: The 1,3,5-trisubstituted pyrazole derivatives has been successfully synthesized and antifungal activity of the compounds denotes that the series BR-1 to BR-4 is most active compound of the all twenty synthesized compounds. The addition of electronegative group (Br, Cl) at third and fifth position in pyrazole ring may necessary for the activity against fungal strains.
The document describes the synthesis and antimicrobial screening of some pyrazolyl heterocycles. Specifically, it details the synthesis of compounds 3, 4, 5, and 6 through various reactions between 1-phenyl-3-(2-pyridyl)-1H-pyrazole-4-carboxaldehyde and acetophenone derivatives. Compound 3 undergo oxidative cyclization to form compounds 4 and 5. Compound 3 also undergoes condensation with hydrazine to form compound 6. The structures of compounds 3, 4, 5, and 6 were characterized using spectral methods. These compounds were then tested for antimicrobial activity against various bacteria and fungi, with some compounds showing moderate to good activity.
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
All manuscripts are subject to rapid peer review. Those of high quality (not previously published and not under consideration for publication in another journal) will be published without delay.
Design, synthesis, characterization and biological evaluation of 3- (4-(7-chl...iosrjce
Novel thiazolidinone derivatives TQ-VI(1-10) were designed, synthesized and screened for
antimicrobial activity. Synthesis of 3-(4-(7-chloro-2-(4-chlorophenyl) 4-oxo-quinazolin-3(4H)-yl) phenyl) -
2-arylthiazolidin-4-one TQ-VI(1-10) have been achieved from the starting material 2-amino-4-chlorobenzoic
acid TQ-I on cyclization with p-chlorobenzoyl chloride TQ-II to yield 7-chloro-2-(4-chlorophenyl)-4H-3,1-
benzoxazin-4-one,TQ-III, which on treatment with p-phenylindiamine gave 3-(4-aminophenyl)-7-chloro-2-(4-
chlorophenyl)quinazolin-4(3H)-one, TQ-IV in good yield. Then, TQ-IV on reaction with substituted aromatic
aldehydes converted to TQ-V(1-10), which on cyclization with thioglycolic acid gave TQ-VI (1-10). All the
synthesized compounds have been characterized on the basis of IR,
1
H-NMR and mass spectral data. The
compounds containing 4-OH, 4-OCH3 and 3,4,5-(OCH3)3 showed good activity. The title compounds were
screened for qualitative (zone of inhibition) and quantitative antimicrobial activity (MIC) by agar cup plate
method and serial dilution technique, respectively. Among the synthesized compounds in the series, the
compound TQVI4 and TQVI5 were found to exhibit significant antifungal activity at lower concentration of
31.25 µg/ml, against A.niger. The compound TQVI5 and TQVI4 showed zone of inhibition of 17mm and 15mm
against A.niger and C.albicans respectively which is comparable to that of standard drug. The rest of the
analogues in the series displayed weak to moderate antimicrobial activity when compared to the standard
positive controls Ampicillin and Amphotericin B.
This document describes the synthesis and characterization of new substituted 1,3,5-triazine compounds containing 1,2,4-triazole and substituted urea/thiourea. The compounds were synthesized in three steps and characterized using techniques such as IR, 1H NMR and elemental analysis. Some of the synthesized compounds (1c, 1e, 1g) showed excellent antimicrobial activity against test microorganisms. The document provides experimental details on the synthesis of the compounds and evaluates their potential as antimicrobial agents.
1. The document describes the synthesis and characterization of new substituted 1,3,5-triazine compounds containing 1,2,4-triazole and substituted urea/thiourea groups.
2. These compounds were synthesized in a stepwise manner and characterized using techniques like IR, NMR and elemental analysis.
3. The antimicrobial activity of the synthesized compounds was evaluated against various microorganisms, with some compounds like 1c, 1e and 1g showing excellent activity.
This document describes the synthesis of 17 new 1,2,4-triazole derivatives and evaluates their antimicrobial and anticancer activities. The compounds showed the most potent antimicrobial activity against the fungus Aspergillus niger. Compound 14 was the most active. Compound 7 exhibited appreciable anticancer activity against colon cancer cells. Quantitative structure-activity relationship analysis identified topological and electronic properties important for the compounds' antimicrobial effects.
Synthesis, characterization and biological activities of novel 2-mercaptobenz...ijperSS
ABSTRACT
A new series of Benzoxazol-2-ylthio-N-(4-substituted) acetohydrazide derivatives (IVa-IVk), were obtained by synthesising new Schiff’s bases derived from benzoxolyl-2-mercaptoaceto hydrazide derivatives by treating with various aryl/hetero aryl aldehydes. Their chemical structures have been confirmed by 1H-NMR, 13C-NMR, FT-IR and ESI-MS spectral data. The synthesised derivatives (IVa-IVk) were screened for their in vitro antimicrobial activities by agar diffusion method. Among the synthesized compounds IVb, IVe, and IVk shown strong antibacterial activity and the compounds IVb, IVe and IVf exhibited strong antifungal activity.
Key words: Benzoxazole, aryl/hetero aryl aldehydes, schiff’s bases, antibacterial activity, antifungal activity.
Ijpar 14 618 ashaSynthesis and screening of new 2-(2-oxoindoline-3-ylidene)-n...pharmaindexing
This document describes the synthesis and characterization of new 2-(2-oxoindoline-3-ylidene)-N-phenyl hydrazine carbothioamide derivatives and evaluation of their antimicrobial activity. It involves a three step synthesis of the derivatives from aryl amines, including purification and characterization of intermediates and final compounds. The compounds were characterized using physical methods like melting point and spectroscopy. The compounds were evaluated for antibacterial activity against four bacteria and antifungal activity against two fungi using disk diffusion assays. Some of the compounds showed good antimicrobial activity.
The document summarizes a study that evaluated (4Z)-2,5-dimethyl-4-(4-methylpyrimido[1,2-a]benzimidazol-2(1H)-ylidene)-2,4-dihydro-3H-pyrazol-3-one (P1) as a corrosion inhibitor for mild steel in 1 M HCl solution using various experimental techniques and quantum chemical calculations. The inhibition efficiency of P1 was found to increase with increasing concentration and was well described by the Langmuir adsorption model. Polarization, electrochemical impedance spectroscopy, and weight loss measurements showed that P1 acts as an effective corrosion inhibitor for mild steel in HCl
This document describes a study on using a solid silica-based sulfonic acid catalyst for the one-pot synthesis of 2H-indazolo[2,1-b]phthalazine-trione derivatives. Key points:
1) A novel and efficient one-pot method is reported that uses a solid silica-based sulfonic acid heterogeneous and reusable catalyst under thermal and solvent-free conditions.
2) This method has advantages of high yields, a cleaner reaction, simple methodology, easy work-up and greener conditions.
3) The catalyst is easily prepared, stable up to 300°C, reusable and efficient under the reaction conditions studied.
This document describes a study that developed a novel method for synthesizing 2H-indazolo[2,1-b]phthalazine-trione derivatives using solid silica-based sulfonic acid as a heterogeneous reusable catalyst. The method has advantages such as high yields, cleaner reactions, simple methodology, easy work-up, and greener conditions. The catalyst is easily prepared, stable up to 300°C, reusable, and efficient under reaction conditions. The study evaluated different catalysts and reaction temperatures to optimize the process. The optimized method uses dimedone, phthalhydrazide, an aromatic aldehyde, and solid silica-based sulfonic acid at 100°C to produce the desired products in
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
Synthesis and antimicrobial activity of some methyl (4- (benzo[d]oxazol-2-yl)...QUESTJOURNAL
1. A series of methyl (4-(benzo[d]oxazol-2-yl)phenyl) carbamodithioate amine derivatives were synthesized by reacting methyl (4-(benzo[d]oxazol-2-yl)phenyl) carbamodithioate with various amines.
2. The synthesized compounds were screened for their in vitro growth inhibiting activity against bacteria and fungi. Compounds exhibited moderate to high antibacterial and antifungal activity.
3. The structures of the compounds were characterized using spectral data such as IR, NMR, mass spectrometry, and elemental analysis. The compounds were then tested for their antimicrobial properties against various bacteria and fungi.
STUDIES ON TREATMENT OF PHARMACEUTICAL WASTE EFFLUENTS BY POLYMER MATERIALS M...EDITOR IJCRCPS
In the present study, sorption technique was used to achieve the optimum recovery of the pharmaceutical waste from effluents.
The modified urea formaldehyde resin was prepared and mixed with inorganic adsorbent at various proportions. The removal
capabilities of pharmaceutical waste by the prepared composite materials were investigated. Different factors affecting the uptake
such as contact time, pH value and aqueous volume to resin weight ratio have been investigated. The reaction mechanisms and
the optimum conditions for the treatment were deduced in the light of the obtained results.
Keywords: Sorption technique, Pharmaceutical waste, Different factors.
This is an Engg Biotechnology project based on medicinal plant i.e singapore cherry or jamaican cherry tree (scientific name Muntingia calabure ), we did in 2013 in GMIT college Davangere, karanataka, India. i have complete project detail what we did..,
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
ER Publication,
IJETR, IJMCTR,
Journals,
International Journals,
High Impact Journals,
Monthly Journal,
Good quality Journals,
Research,
Research Papers,
Research Article,
Free Journals, Open access Journals,
erpublication.org,
Engineering Journal,
Science Journals,
Design, Synthesis, and Characterization of New 1,3,5-Trisubstituted-2-pyrazol...BRNSS Publication Hub
Objective: The objective of the paper was to design, synthesis, and characterization of new 1,3,5-trisubstituted-2-pyrazolines derivative and to evaluate for analgesic potential. Materials and Methods: The 1,3,5-tri-substituted-2-pyrazolines derivatives have been synthesized by the reaction of chalcone derivatives with 4-hydrazinylbenzene sulfonamide hydrochloride and phenyl hydrazine hydrochloride. Total 16 compounds have been synthesized and characterized by the IR, 1HNMR, and mass spectral analysis. Proposed compounds have been evaluated for analgesic activity. The synthesized compounds also evaluated for the analgesic activity by the following two methods, that is, hot plate test method and acetic acid induced writhing in mice. Pentazocine and acetyl acetic acid were used as standard drug for compare the efficacy. Results and Discussion: The analgesic activity of the 16 synthesized compound series A1-A8, and B1-B8 has been evaluated using hot plate test method and acetic acid induced writhing in mice. The results of the evaluation have been viewed by taking pentazocine and acetyl acetic acid as the standard drug. In hot plate test, series A1-A8, shown delay the paw withdrawal latency time for compound A2 (10.30 s), A4 (9.45 s), A7 (11.65 s), and A8 (11.26 s) after 90 min. In series, B1-B8 shown delay the paw withdrawal latency time for compound B2 (9.10 s) and B7 (10.42 s) after 90 min, inhibit the pain sensation, and inhibit pain produced by thermal means. Synthesized compounds of series A1-A8, compounds A2, A5, A6, A7, and A8 were shown 83.00, 76.01, 80.34, 86.99, and 88.15 were shown percent inhibition, significantly (p<0.05 and p<0.001, respectively) and reduced the number of wriths induced by 0.6% acetic acid at the dose of 10 mg/kg. Acetylsalicylic acid (10 mg/kg) appears to be better effective in reducing the number of wriths, it significantly (P < 0.001) reduced the number of wriths by 99.0%. The compounds B1, B3, and B4 have shown least active activity. These all finding suggest that these synthesized compounds have the potential as analgesic agent. Conclusion: The 1,3,5-pyrazoline derivatives has been successfully synthesized and evaluated for analgesic activity of mice model and results data indicate that compounds A2, A5, A6, A7, and A8 were shown 83.00, 76.01, 80.34, 86.99, and 88.15%, and compounds B2, B7, and B8 were shown 72.25, 74.27, and 74.56% inhibitions. The presence of SO2NH2 is essential for analgesic activity.
Synthesis, characterization of certain new heterocyclic hybrids of pyrazoles ...SriramNagarajan15
The document describes the synthesis and characterization of novel pyrazole derivatives and their evaluation for anti-inflammatory activity. Various pyrazole derivatives were synthesized by reacting hydrazides with acetyl acetone. The structures of the intermediates and final compounds were confirmed using IR, NMR, mass spectroscopy. The compounds were evaluated for anti-inflammatory activity using carrageenan induced paw edema method. Some compounds showed significant anti-inflammatory activity comparable to the reference drug ibuprofen. The synthesized derivatives could be further studied for their clinical efficacy as anti-inflammatory agents.
This document compares different methods for assaying hyaluronidase enzyme preparations, including a biological skin diffusion assay and two physicochemical assays (viscosimetric and turbidimetric). Seven different hyaluronidase preparations were assayed using all three methods. The results showed reasonable correlation between the biological assay and viscosimetric assay, but poorer correlation with the turbidimetric assay. The nature of the hyaluronate substrate did not significantly affect the viscosimetric assay results for most preparations, except one streptococcal preparation which showed higher activity on purified substrate.
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.
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.
DPPH Scavenging Assay of Eighty Four Bangladeshi Medicinal PlantsIOSR Journals
This study was designed to screen out free radical scavenging potentiality of 84 medicinal plants. Stock solution of different plant extracts and standard were diluted to achieve suitable concentrations. A control was also prepared without plant extract solution. Then 0.004% DPPH solution was added. The mixtures were incubated in the room temperature for 30 minutes. Then the absorbance was measured at 517 nm against solvent in UV-spectrophotometer and then IC50 was calculated. In this experiment two standard were used-ascorbic acid and BHT. Both showed a significant IC50 value of 15.5μg/mL, and 46.54μg/mL respectively. Among 84 medicinal plants Syzygim cumini, Casuarina littorea, Borassus flabellifer, Enhydra fluctuans, and Minusops elengi exhibited highest radical scavenging potential with an IC50 value of 12.816μg/mL, 14.467μg/mL, 15.755μg/mL, 15.653μg/mL, and 20.380μg/mL respectively. All these value are very close to the IC50 value of ascorbic acid and better than IC50 value of BHT (Butylated Hydroxy Toluene). Syzygim cumini is the most powerful scavenger among all tested medicinal plants and also most strong scavenger than ascorbic acid and BHT. Scavenging activity was found to increase in dose dependent manner. Another 30 medicinal plants exhibited good scavenging property and 14 medicinal plants showed moderate scavenging activity. The rest presented lower scavenging activity. This present study indicates that plants having good scavenging property may have various health beneficial effects and these plants can be considered as valuable source of bioactive components with high antioxidant properties.
This document summarizes the synthesis and characterization of diorganotin(IV) complexes with three hydrazone ligands. Specifically, it discusses the synthesis of diorganotin(IV) complexes with the ligands N0
-(5-bromo-2-hydroxybenzy-lidene) isonicotinohydrazide (H2La
), N0
-((2-hydroxynaphthalen-1-yl)methylene) isonicotinohydrazide (H2Lb
) and N0
-(2,4-dihydroxybenzylidene) isonicotinohydrazide (H2Lc
) and
A STUDY TO EVALUATE THE IN VITRO ANTIMICROBIAL ACTIVITY AND ANTIANDROGENIC E...Dr. Pradeep mitharwal
The present paper deals with synthesis and characterization
of some new chromium (III) Schiff base complexes using microwave irradiation
technique as well as conventional heating. The S∩N donor benzothiazolines, 1-
(2-furanyl) ethanone benzothiazoline (Bzt1N
∩
SH), 1-(2-thienyl) ethanone
benzothiazoline (Bzt2N
∩
SH) and 1-(2-pyridyl) ethanone benzothiazoline
(Bzt3N
∩
SH) were prepared by the condensation of ortho-aminothiophenol with
respective ketones in ethanol.
The document describes the synthesis and testing of novel carboxamide derivatives of 2-quinolones for their antimicrobial and antitubercular activities. A series of 12 derivatives were synthesized by reacting substituted 3-acetyl-1-amino-quinolin-2-one with substituted benzoic acids. The compounds were characterized using IR, NMR and mass spectroscopy. Testing found that several derivatives exhibited promising antibacterial activity against both gram-positive and gram-negative bacteria. Compounds also demonstrated antitubercular activity when tested against Mycobacterium tuberculosis. The results indicate that some of the novel 2-quinolone carboxamide derivatives have potential as antimicrobial and antitubercular agents.
7 synthesis, characterisation and antimicrobial activity of schiff base of 7 ...BIOLOGICAL FORUM
ABSTRACT: Compounds having 2-quinolone moiety are associated with interesting biological activities. In the present study, we synthesized Schiff bases of 7-hydroxy-3-methyl-2-quinolone and their antibacterial activity was evaluated by wells diffusion method. Schiff bases of 7-hydroxy-3-methyl-2-quinolone (1 to 5 named as Q2aa-Q2ae) were prepared by refluxing 7-hydroxy-3-methyl-2-quinolone with substituted aromatic aldehydes. The final test compounds were purified and characterized by IR, 1HNMR and Mass Spectral studies. M.P. of these compounds was confirmed by open capillary method instrument chemline cl 725. They were evaluated for antibacterial activity. Compounds were active against Klebsiella pneumonia and Enterococcus faecalis. While ciprofloxacin was used as standards.
Ijpar 14 618 ashaSynthesis and screening of new 2-(2-oxoindoline-3-ylidene)-n...pharmaindexing
This document describes the synthesis and characterization of new 2-(2-oxoindoline-3-ylidene)-N-phenyl hydrazine carbothioamide derivatives and evaluation of their antimicrobial activity. It involves a three step synthesis of the derivatives from aryl amines, including purification and characterization of intermediates and final compounds. The compounds were characterized using physical methods like melting point and spectroscopy. The compounds were evaluated for antibacterial activity against four bacteria and antifungal activity against two fungi using disk diffusion assays. Some of the compounds showed good antimicrobial activity.
The document summarizes a study that evaluated (4Z)-2,5-dimethyl-4-(4-methylpyrimido[1,2-a]benzimidazol-2(1H)-ylidene)-2,4-dihydro-3H-pyrazol-3-one (P1) as a corrosion inhibitor for mild steel in 1 M HCl solution using various experimental techniques and quantum chemical calculations. The inhibition efficiency of P1 was found to increase with increasing concentration and was well described by the Langmuir adsorption model. Polarization, electrochemical impedance spectroscopy, and weight loss measurements showed that P1 acts as an effective corrosion inhibitor for mild steel in HCl
This document describes a study on using a solid silica-based sulfonic acid catalyst for the one-pot synthesis of 2H-indazolo[2,1-b]phthalazine-trione derivatives. Key points:
1) A novel and efficient one-pot method is reported that uses a solid silica-based sulfonic acid heterogeneous and reusable catalyst under thermal and solvent-free conditions.
2) This method has advantages of high yields, a cleaner reaction, simple methodology, easy work-up and greener conditions.
3) The catalyst is easily prepared, stable up to 300°C, reusable and efficient under the reaction conditions studied.
This document describes a study that developed a novel method for synthesizing 2H-indazolo[2,1-b]phthalazine-trione derivatives using solid silica-based sulfonic acid as a heterogeneous reusable catalyst. The method has advantages such as high yields, cleaner reactions, simple methodology, easy work-up, and greener conditions. The catalyst is easily prepared, stable up to 300°C, reusable, and efficient under reaction conditions. The study evaluated different catalysts and reaction temperatures to optimize the process. The optimized method uses dimedone, phthalhydrazide, an aromatic aldehyde, and solid silica-based sulfonic acid at 100°C to produce the desired products in
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
Synthesis and antimicrobial activity of some methyl (4- (benzo[d]oxazol-2-yl)...QUESTJOURNAL
1. A series of methyl (4-(benzo[d]oxazol-2-yl)phenyl) carbamodithioate amine derivatives were synthesized by reacting methyl (4-(benzo[d]oxazol-2-yl)phenyl) carbamodithioate with various amines.
2. The synthesized compounds were screened for their in vitro growth inhibiting activity against bacteria and fungi. Compounds exhibited moderate to high antibacterial and antifungal activity.
3. The structures of the compounds were characterized using spectral data such as IR, NMR, mass spectrometry, and elemental analysis. The compounds were then tested for their antimicrobial properties against various bacteria and fungi.
STUDIES ON TREATMENT OF PHARMACEUTICAL WASTE EFFLUENTS BY POLYMER MATERIALS M...EDITOR IJCRCPS
In the present study, sorption technique was used to achieve the optimum recovery of the pharmaceutical waste from effluents.
The modified urea formaldehyde resin was prepared and mixed with inorganic adsorbent at various proportions. The removal
capabilities of pharmaceutical waste by the prepared composite materials were investigated. Different factors affecting the uptake
such as contact time, pH value and aqueous volume to resin weight ratio have been investigated. The reaction mechanisms and
the optimum conditions for the treatment were deduced in the light of the obtained results.
Keywords: Sorption technique, Pharmaceutical waste, Different factors.
This is an Engg Biotechnology project based on medicinal plant i.e singapore cherry or jamaican cherry tree (scientific name Muntingia calabure ), we did in 2013 in GMIT college Davangere, karanataka, India. i have complete project detail what we did..,
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
ER Publication,
IJETR, IJMCTR,
Journals,
International Journals,
High Impact Journals,
Monthly Journal,
Good quality Journals,
Research,
Research Papers,
Research Article,
Free Journals, Open access Journals,
erpublication.org,
Engineering Journal,
Science Journals,
Design, Synthesis, and Characterization of New 1,3,5-Trisubstituted-2-pyrazol...BRNSS Publication Hub
Objective: The objective of the paper was to design, synthesis, and characterization of new 1,3,5-trisubstituted-2-pyrazolines derivative and to evaluate for analgesic potential. Materials and Methods: The 1,3,5-tri-substituted-2-pyrazolines derivatives have been synthesized by the reaction of chalcone derivatives with 4-hydrazinylbenzene sulfonamide hydrochloride and phenyl hydrazine hydrochloride. Total 16 compounds have been synthesized and characterized by the IR, 1HNMR, and mass spectral analysis. Proposed compounds have been evaluated for analgesic activity. The synthesized compounds also evaluated for the analgesic activity by the following two methods, that is, hot plate test method and acetic acid induced writhing in mice. Pentazocine and acetyl acetic acid were used as standard drug for compare the efficacy. Results and Discussion: The analgesic activity of the 16 synthesized compound series A1-A8, and B1-B8 has been evaluated using hot plate test method and acetic acid induced writhing in mice. The results of the evaluation have been viewed by taking pentazocine and acetyl acetic acid as the standard drug. In hot plate test, series A1-A8, shown delay the paw withdrawal latency time for compound A2 (10.30 s), A4 (9.45 s), A7 (11.65 s), and A8 (11.26 s) after 90 min. In series, B1-B8 shown delay the paw withdrawal latency time for compound B2 (9.10 s) and B7 (10.42 s) after 90 min, inhibit the pain sensation, and inhibit pain produced by thermal means. Synthesized compounds of series A1-A8, compounds A2, A5, A6, A7, and A8 were shown 83.00, 76.01, 80.34, 86.99, and 88.15 were shown percent inhibition, significantly (p<0.05 and p<0.001, respectively) and reduced the number of wriths induced by 0.6% acetic acid at the dose of 10 mg/kg. Acetylsalicylic acid (10 mg/kg) appears to be better effective in reducing the number of wriths, it significantly (P < 0.001) reduced the number of wriths by 99.0%. The compounds B1, B3, and B4 have shown least active activity. These all finding suggest that these synthesized compounds have the potential as analgesic agent. Conclusion: The 1,3,5-pyrazoline derivatives has been successfully synthesized and evaluated for analgesic activity of mice model and results data indicate that compounds A2, A5, A6, A7, and A8 were shown 83.00, 76.01, 80.34, 86.99, and 88.15%, and compounds B2, B7, and B8 were shown 72.25, 74.27, and 74.56% inhibitions. The presence of SO2NH2 is essential for analgesic activity.
Synthesis, characterization of certain new heterocyclic hybrids of pyrazoles ...SriramNagarajan15
The document describes the synthesis and characterization of novel pyrazole derivatives and their evaluation for anti-inflammatory activity. Various pyrazole derivatives were synthesized by reacting hydrazides with acetyl acetone. The structures of the intermediates and final compounds were confirmed using IR, NMR, mass spectroscopy. The compounds were evaluated for anti-inflammatory activity using carrageenan induced paw edema method. Some compounds showed significant anti-inflammatory activity comparable to the reference drug ibuprofen. The synthesized derivatives could be further studied for their clinical efficacy as anti-inflammatory agents.
This document compares different methods for assaying hyaluronidase enzyme preparations, including a biological skin diffusion assay and two physicochemical assays (viscosimetric and turbidimetric). Seven different hyaluronidase preparations were assayed using all three methods. The results showed reasonable correlation between the biological assay and viscosimetric assay, but poorer correlation with the turbidimetric assay. The nature of the hyaluronate substrate did not significantly affect the viscosimetric assay results for most preparations, except one streptococcal preparation which showed higher activity on purified substrate.
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.
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.
DPPH Scavenging Assay of Eighty Four Bangladeshi Medicinal PlantsIOSR Journals
This study was designed to screen out free radical scavenging potentiality of 84 medicinal plants. Stock solution of different plant extracts and standard were diluted to achieve suitable concentrations. A control was also prepared without plant extract solution. Then 0.004% DPPH solution was added. The mixtures were incubated in the room temperature for 30 minutes. Then the absorbance was measured at 517 nm against solvent in UV-spectrophotometer and then IC50 was calculated. In this experiment two standard were used-ascorbic acid and BHT. Both showed a significant IC50 value of 15.5μg/mL, and 46.54μg/mL respectively. Among 84 medicinal plants Syzygim cumini, Casuarina littorea, Borassus flabellifer, Enhydra fluctuans, and Minusops elengi exhibited highest radical scavenging potential with an IC50 value of 12.816μg/mL, 14.467μg/mL, 15.755μg/mL, 15.653μg/mL, and 20.380μg/mL respectively. All these value are very close to the IC50 value of ascorbic acid and better than IC50 value of BHT (Butylated Hydroxy Toluene). Syzygim cumini is the most powerful scavenger among all tested medicinal plants and also most strong scavenger than ascorbic acid and BHT. Scavenging activity was found to increase in dose dependent manner. Another 30 medicinal plants exhibited good scavenging property and 14 medicinal plants showed moderate scavenging activity. The rest presented lower scavenging activity. This present study indicates that plants having good scavenging property may have various health beneficial effects and these plants can be considered as valuable source of bioactive components with high antioxidant properties.
This document summarizes the synthesis and characterization of diorganotin(IV) complexes with three hydrazone ligands. Specifically, it discusses the synthesis of diorganotin(IV) complexes with the ligands N0
-(5-bromo-2-hydroxybenzy-lidene) isonicotinohydrazide (H2La
), N0
-((2-hydroxynaphthalen-1-yl)methylene) isonicotinohydrazide (H2Lb
) and N0
-(2,4-dihydroxybenzylidene) isonicotinohydrazide (H2Lc
) and
A STUDY TO EVALUATE THE IN VITRO ANTIMICROBIAL ACTIVITY AND ANTIANDROGENIC E...Dr. Pradeep mitharwal
The present paper deals with synthesis and characterization
of some new chromium (III) Schiff base complexes using microwave irradiation
technique as well as conventional heating. The S∩N donor benzothiazolines, 1-
(2-furanyl) ethanone benzothiazoline (Bzt1N
∩
SH), 1-(2-thienyl) ethanone
benzothiazoline (Bzt2N
∩
SH) and 1-(2-pyridyl) ethanone benzothiazoline
(Bzt3N
∩
SH) were prepared by the condensation of ortho-aminothiophenol with
respective ketones in ethanol.
The document describes the synthesis and testing of novel carboxamide derivatives of 2-quinolones for their antimicrobial and antitubercular activities. A series of 12 derivatives were synthesized by reacting substituted 3-acetyl-1-amino-quinolin-2-one with substituted benzoic acids. The compounds were characterized using IR, NMR and mass spectroscopy. Testing found that several derivatives exhibited promising antibacterial activity against both gram-positive and gram-negative bacteria. Compounds also demonstrated antitubercular activity when tested against Mycobacterium tuberculosis. The results indicate that some of the novel 2-quinolone carboxamide derivatives have potential as antimicrobial and antitubercular agents.
7 synthesis, characterisation and antimicrobial activity of schiff base of 7 ...BIOLOGICAL FORUM
ABSTRACT: Compounds having 2-quinolone moiety are associated with interesting biological activities. In the present study, we synthesized Schiff bases of 7-hydroxy-3-methyl-2-quinolone and their antibacterial activity was evaluated by wells diffusion method. Schiff bases of 7-hydroxy-3-methyl-2-quinolone (1 to 5 named as Q2aa-Q2ae) were prepared by refluxing 7-hydroxy-3-methyl-2-quinolone with substituted aromatic aldehydes. The final test compounds were purified and characterized by IR, 1HNMR and Mass Spectral studies. M.P. of these compounds was confirmed by open capillary method instrument chemline cl 725. They were evaluated for antibacterial activity. Compounds were active against Klebsiella pneumonia and Enterococcus faecalis. While ciprofloxacin was used as standards.
Synthesis, Characterization, Biological Evaluation of Some Heterocyclic Oxaze...JapaneseJournalofGas
The new serious of pentyloxy and aryloxy benzaldehyde (3ae) were synthesized from the substitution reaction of 4-hydroxy benzaldehyde with different aryl bromide and alkyl bromide, on the basis of Williamson ether synthesis in the presence of Potassium carbonate using absolute ethanol as a solvent. The second step was the synthesis of 2-amino-5-(p-tolyl)1,3,4-thiadiazole.
Synthesis, Characterization, Biological Evaluation of Some Heterocyclic Oxaze...JohnJulie1
The new serious of pentyloxy and aryloxy benzaldehyde (3ae) were synthesized from the substitution reaction of 4-hydroxy benzaldehyde with different aryl bromide and alkyl bromide, on the basis of Williamson ether synthesis in the presence of Potassium carbonate using absolute ethanol as a solvent. The second step was the synthesis of 2-amino-5-(p-tolyl)1,3,4-thiadiazole.
This document describes the design, synthesis, and evaluation of new 1,3,5-trisubstituted-2-pyrazoline derivatives for their analgesic potential. Sixteen compounds were synthesized via the reaction of chalcone derivatives with 4-hydrazinylbenzenesulfonamide hydrochloride or phenylhydrazine hydrochloride. The compounds were characterized using techniques such as IR, NMR, and mass spectroscopy. The compounds were evaluated for analgesic activity using hot plate test and acetic acid-induced writhing tests in mice. Several compounds showed significant analgesic activity in both tests compared to standard drugs. The presence of the SO2NH2 group was found to be important for analgesic activity
Synthesis, Characterization and Biological Evaluation of Oxazolone Derivativesijceronline
A series of six 4-aryl Benzelidene-2-phenyl-5- oxazolone derivatives were synthesized by condensation of aromatic aldehydes with N-benzoyl glycine (Hippuric acid) in the presence of sodium acetate and acetic anhydride at room temperature in ethanol. Six of the compounds are new derivatives. The structures of the compounds were evaluated based on 1H-NMR , IR and FTIR methods and by elemental analysis. .All the derivative compounds prepared were tested for their antimicrobial activity by disk diffusion technique. Test organisms: Bacteria like Staphylococcus aureusMTCC 7443 and Salmonella typhimuriumMTCC 733 Fungi like C.albicans and A.flavus The results were compared with those of the standard 0.5% Ciprofloxacin. The derivatives with Salicylaldehyde and cinnamaldehyde were showed excellent activities against E. coli. and Staphylococcus aureusMTCC 7443 : than Salmonella typhimuriumMTCC 733 bacteria. It also showed reasonable activity withFungi like C.albicans than A.flavus
Synthesis and Anti-inflammatory activity of 2-amino-6-methoxy benzothiazole d...IOSR Journals
This document describes the synthesis and anti-inflammatory activity of 2-amino-6-methoxy benzothiazole derivatives. Two compounds were synthesized through simple condensation reactions and characterized using analytical techniques. These compounds were then screened for their anti-inflammatory activity and showed satisfactory inhibition of haemolysis compared to the standard drug. The hydrazino derivative showed better anti-inflammatory results than the intermediate compound.
Synthesis and Anti-Inflammatory activity of Sulpha/substituted 1,2-Diazolesinventionjournals
A Novel compound namely N1 (3 Nicotinoyl) 3,5 dimethyl-4-(N-4-sulfamoyl-azo)-1,2-diazoles has been synthesized by two step processes. Synthesis of N1 -4-sulfamoylphenylhydrazono-3,5-dimethyl propane-1,3-dione and sulfonamide, which interacting with 3-Nicotinoyl hydrazine to form final compound. The newly synthesized compound N1 -(3-Nicotinoyl)-3,5-dimethyl 4-(N1 -4-sulfamoyl phenyl azo) 1,2-diazoles was screened for antiinflammatory activity
Synthesis and Anti-Inflammatory activity of Sulpha/substituted 1,2-Diazolesinventionjournals
A Novel compound namely N1 (3 Nicotinoyl) 3,5 dimethyl-4-(N-4-sulfamoyl-azo)-1,2-diazoles has been synthesized by two step processes. Synthesis of N1 -4-sulfamoylphenylhydrazono-3,5-dimethyl propane-1,3-dione and sulfonamide, which interacting with 3-Nicotinoyl hydrazine to form final compound. The newly synthesized compound N1 -(3-Nicotinoyl)-3,5-dimethyl 4-(N1 -4-sulfamoyl phenyl azo) 1,2-diazoles was screened for antiinflammatory activity
This document summarizes the synthesis and evaluation of various N-substituted 5-[(4-chlorophenoxy)methyl]-1,3,4-oxadiazole-2yl-2-sulfanyl acetamides. It describes a multi-step synthesis starting with 4-chlorophenoxyacetic acid and involving esterification, hydrazide formation, and cyclization to form the core 1,3,4-oxadiazole ring. This intermediate was then reacted with various N-substituted bromoacetamides to yield the target compounds. The compounds were characterized using spectral methods and evaluated for antibacterial activity, inhibition of alpha-chymotrypsin enzyme, and cytotoxic
1. A new Schiff base ligand was synthesized by condensing amoxicillin and 4-(dimethylamino)benzaldehyde. Mixed ligand complexes were synthesized from reactions of the Schiff base ligand with metal salts such as Fe(II), Co(II), Ni(II), Cu(II), and Zn(II) along with nicotinamide.
2. The complexes were characterized using various techniques such as elemental analysis, FT-IR, UV-Vis, magnetic susceptibility measurements, and evaluating their conductivities. The data indicated the complexes had octahedral geometries and were non-electrolytes.
3. The antimicrobial activities of the complexes were evaluated against various bacteria and found to have
1. A new Schiff base ligand was synthesized from amoxicillin and 4-(dimethylamino)benzaldehyde. Mixed ligand complexes were synthesized from reactions of the ligand with Fe(II), Co(II), Ni(II), Cu(II), and Zn(II) and nicotinamide in a 1:1:2 ratio.
2. The ligand and complexes were characterized using various spectroscopic and analytical techniques. Octahedral geometries were suggested for the complexes.
3. The antimicrobial activities of the complexes were evaluated against various bacterial species and found to have enhanced activity compared to the uncomplexed ligand.
The document describes the synthesis and characterization of 20 new 1,3,5-trisubstituted pyrazole derivatives and their evaluation for antifungal activity. The derivatives were synthesized by reacting chalcone derivatives with succinic hydrazide in pyridine. The derivatives were characterized using IR, 1H NMR, and mass spectroscopy. The compounds were evaluated for antifungal activity against four fungal strains at two concentrations using an agar diffusion method. Several of the compounds showed mild to good antifungal activity, with the BR series (BR-1 to BR-4) being the most active. The presence of electronegative groups like Br and Cl at the third and fifth positions of the py
This document describes the synthesis and characterization of cyanopyridine derivatives and their evaluation for antitubercular and anthelmintic activity. Chalcones were first synthesized through Claisen-Schmidt condensation and then reacted with malononitrile to obtain cyanopyridines. The structures of the compounds were characterized using techniques such as IR, NMR and mass spectrometry. The cyanopyridines were then evaluated for antitubercular activity against M. tuberculosis using the microplate Alamar Blue assay and for anthelmintic activity against earthworms. Some of the compounds showed promising activity in both assays.
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
Synthesis, Characterization and Biological evaluation of substituted Pyrazole...SriramNagarajan15
The work presented in this article consists of synthesis, characterization and biological evaluation of substituted pyrazole derivatives. Pyrazole derivatives have been shown to have wide variety of pharmacological activities like antimicrobial, antiviral, antihistaminic, antitumor, antipyretic, anti-inflammatory, antidepressant and anticonvulsant. As combination of biologically active moieties into one molecule and synthesis of totally newer moieties have been the methods of research, we present here synthesis of some novel pyrazole derivatives incorporating various biologically active aryl/aryloxy acid derivatives such as ibuprofen, diclofenac, aceclofenac as well as potent antibacterial quinolones, norfloxacin and ciprofloxacin. All the compounds synthesized were evaluated for their antimicrobial activity.
Design, Synthesis, Biological Evaluation, and In Silico ADMET Studies of 1,8-...BRNSS Publication Hub
In the present study, 1,8-naphthyridine-3-carboxylic acid derivatives (5a1, 5a2, 5b1, and 5b2) were
designed, synthesized, and screened for their in vitro H1-antihistaminic activity. H1R inhibitory activity
of the synthesized derivatives was calculated by the modified Van Arman technique, histamine-induced
bronchoconstriction in guinea pigs. A good bronchorelaxant effect of compounds was observed in
histamine-contracted guinea pig tracheal chain through H1-receptor antagonism. In addition, the
hypothetically resulted compounds are checked for their reliability on other in silico drug designing
online web services like SwissADME predictor. In silico ADMET analysis results show that all the
derivatives had negligible toxicity, good absorption, and solubility profile. These compounds may serve
as possible lead for establishing safe and effective antihistaminic agent(s).
Synthesis and pharmacological evaluation of novel imidazole derivativespharmaindexing
This document summarizes a research study that synthesized novel imidazole derivatives and evaluated their pharmacological properties. Specifically:
- Seven novel imidazole derivatives containing an imidazole-isatin scaffold were synthesized. Their structures and physical properties were characterized.
- The compounds were evaluated for anthelmintic activity using Pheretima posthuma earthworms as a model. The time taken for paralysis and death of the worms was recorded and compared to the reference drug albendazole.
- One of the synthesized compounds, 2-(1H-imidazol-1-yl)-N’-(2-oxoindolin-3-ylidene)acetohydra
The document describes the synthesis and evaluation of new derivatives of (E)-3-(5-((substitutedphenylamino)methyl)-1,3,4-thiadiazol-2-yl)-2-styryl quinazolin-4(3H)-one as potential antifungal and antibacterial agents. Fifteen derivatives were synthesized by reacting 2-substituted benzoxazin-4-one with (E)-2-(4-substituedstyryl)-4H-benzo[d][1,3]oxazin-4-one. The derivatives were characterized using infrared, 1H NMR and mass spectroscopy. The derivatives were evaluated for antibacterial activity against 4 bacterial
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.
Does Over-Masturbation Contribute to Chronic Prostatitis.pptxwalterHu5
In some case, your chronic prostatitis may be related to over-masturbation. Generally, natural medicine Diuretic and Anti-inflammatory Pill can help mee get a cure.
10 Benefits an EPCR Software should Bring to EMS Organizations Traumasoft LLC
The benefits of an ePCR solution should extend to the whole EMS organization, not just certain groups of people or certain departments. It should provide more than just a form for entering and a database for storing information. It should also include a workflow of how information is communicated, used and stored across the entire organization.
Mercurius is named after the roman god mercurius, the god of trade and science. The planet mercurius is named after the same god. Mercurius is sometimes called hydrargyrum, means ‘watery silver’. Its shine and colour are very similar to silver, but mercury is a fluid at room temperatures. The name quick silver is a translation of hydrargyrum, where the word quick describes its tendency to scatter away in all directions.
The droplets have a tendency to conglomerate to one big mass, but on being shaken they fall apart into countless little droplets again. It is used to ignite explosives, like mercury fulminate, the explosive character is one of its general themes.
Osteoporosis - Definition , Evaluation and Management .pdfJim Jacob Roy
Osteoporosis is an increasing cause of morbidity among the elderly.
In this document , a brief outline of osteoporosis is given , including the risk factors of osteoporosis fractures , the indications for testing bone mineral density and the management of osteoporosis
Travel vaccination in Manchester offers comprehensive immunization services for individuals planning international trips. Expert healthcare providers administer vaccines tailored to your destination, ensuring you stay protected against various diseases. Conveniently located clinics and flexible appointment options make it easy to get the necessary shots before your journey. Stay healthy and travel with confidence by getting vaccinated in Manchester. Visit us: www.nxhealthcare.co.uk
1. International Journal of Pharmaceutical Science Invention
ISSN (Online): 2319 – 6718, ISSN (Print): 2319 – 670X
www.ijpsi.org Volume 3 Issue 6 ‖ June 2014 ‖ PP.27-31
www.ijpsi.org 27 | Page
Synthesis, Characterization and Biological Evaluation Of Some
Novel 2-[(5-Aryl)-4,5-Dihydro-1H-Pyrazole-3-Yl]-1H-
Benzimidazoles As Potential Antimicrobial Agents
Ravinder Reddy Kunduru1
, Malla Reddy Vanga1
*, Srinivas Boche2
1
Dr. Ravishankar memorial Research Laboratory, University College of Pharmaceutical Sciences, Kakatiya
University, Warangal 506009, Telangana, India.
2
Department of Chemistry, Kakatiya University, Warangal 506009, Telangana, India.
ABSTRACT: Various novel 2-[(5-aryl)-4,5-dihydro-1H-pyrazole-3-yl]-1H-benzimidazoles (6a-h) have been
synthesized from 1-(1H-benzimidazol-2-yl)-3-(substituted phenyl) prop-2-en-1-ones (5a-h) by suing different o-
phenylenediamines (1a-d) and lactic acid 2 as starting materials and by involving 2-(α-hydroxy)ethyl
benzimidazoles (3a-d) and 2-acetyl benzimidazoles (4a-d) as intermediates. The chemical structures of these
compounds have been established by IR, 1
H-NMR and Mass spectral data. The newly synthesized compounds
were screened for their ability towards antimicrobial activity.
KEY WORDS: Pyrazoles, benzimidazolines, antimicrobial activity
I. INTRODUCTION:
The resistance to antimicrobial drugs is widespread, the development of new antimicrobial agents and
understanding their mechanism of action are becoming vital nowadays.1
The incorporation of the benzimidazole
nucleus is an important synthetic strategy in studies of antimicrobial drug discovery.2
Benzimidazoles have been
an important pharmacophores and privileged structures in medicinal chemistry,3
encompassing a diverse range
of biological activities including anticancer,4
cytotoxic,5
antihypertensive,6
antiviral,7
vasodilator,8
anti-
arrhythmic, antiulcer, anthelmintical, inotropic, antihistamine, antifungal, anti-inflammatory.9
However many
strategies are available for benzimidazole synthesis.10-14
The exploitation of a simple molecule with different
functionalities for the synthesis of heterocyclics is a worthwhile contribution in the heterocyclic chemistry. The
pyrazoles are prominent nitrogen-containing heterocyclics and, therefore, various procedures have been worked
out for their synthesis.15
Numerous pyrazoles and their derivatives have been found to possess useful bioactivity
such as antihyperglycemic, analgesic, anti-inflammatory, antipyretic, antibacterial, hypoglycemic, sedative-
hypnotic activity,16-22
antimicrobial,23
central nervous system24
and immunosuppressive.25
II. RESULTS AND DISCUSSION:
The therapeutic importance of these rings prompted us to develop selective molecules in which a
substituent could be arranged in a pharmacophoric pattern to display higher pharmacological activities. Thus we
have designed and synthesized a series of novel 2-[(5-aryl)-4,5-dihydro-1H-pyrazole-3-yl]-1H-benzimidazoles
(6a-h) in good to excellent yields by using commercially available o-phenylenediamines (1a-d) and lactic acid 2
(Scheme 1). The synthetic route leading to the title compounds is summarized in scheme 1. The initial
intermediate, 2-(α-hydroxy)ethyl benzimidazoles (3a-d) was prepared through cyclization between o-
phenylenediamines (1a-d) and lactic acid 2 in HCl solution under reflux for 25-26 h. The compound 3a-d was
turned into the intermediate, 2-acetyl benzimidazoles (4a-d) on oxidation with K2Cr2O7 in presence of H2SO4 at
ambient temperature on uniform stirring for 4-5. The final intermediate, 1-(1H-benzimidazol-2-yl)-3-
(substituted phenyl) prop-2-en-1-ones (5a-h) has been prepared from the reaction between compound 4a-d and
different aromatic aldehydes in alkaline medium (60% KOH) by using ethanol solvent on constant stirring at
room temperature for 3-4 h. The title compounds, 2-[(5-aryl)-4,5-dihydro-1H-pyrazole-3-yl]-1H-benzimidazoles
(6a-h) have been prepared from the subsequent ring closure reaction of compound 5a-h with hydrazine hydrate
in acetic acid at reflux temperature for 5-6 h. The chemical structures of all the newly synthesized compounds
were confirmed by their IR, 1
H-NMR and mass spectral data. Further the compounds 6a-h were used to evaluate
their antimicrobial activity.
2. Synthesis, Characterization And Biological Evaluation…
www.ijpsi.org 28 | Page
N H 2
N H 2
R
+
O H
O H
O (i)
N
H
N
O H
R
(ii)
N
H
N
O
R
(iii)
N
H
N
O
R
R'
N
H
N
N N H
R
R'
(iv )
1 a -d 2 3 a -d 4 a -d
5 a -h
6 a -h
O
H
R'
+
Scheme 1: (i) HCl, reflux, 25-26 h, (ii) K2Cr207, H2SO4, 4-5 h, (iii) EtOH, 60% KOH, 3-4 h, (iv) AcOH, reflux, 5-
6h.
1/3/4a-d R = a) H, b) 4-CH3, c) 4-Cl; d) 4-NO2. 5/6a-h R= a) H, b) H, c) H, d) 4-CH3, e) 4-CH3, f) 4-Cl, g) 4-Cl, h)
4-NO2.
5/6a-h R'= a) H, b) 4-OCH3, c) 3,4-OCH3, d) H, e) 4-C2H5, f) 4-C2H5, g) 4-NO2, h) 4-C2H5.
Table 1: Antimicrobial activity of 2-[(5-aryl)-4,5-dihydro-1H-pyrazole-3-yl]-1H-benzimidazoles (6a-h)
Compound Antibacterial activity Antifungal activity
B. subtilus S. aureus E. coli K. pneumoniae F. oxysporum A. niger
6a 05 05 05 05 02 02
6b 13 13 09 10 05 05
6c 15 15 13 12 04 03
6d 13 15 13 13 05 04
6e 10 09 10 08 03 03
6f 13 13 08 07 04 03
6g 13 15 09 11 05 05
6h 09 09 10 05 03 03
Streptomycin 16 16 16 16 - -
Fluconazole - - - - 06 06
ANTIBACTERIAL ACTIVITY
The in vitro antibacterial activity of the newly synthesized compounds was evaluated against two
representative gram-positive bacteria viz., B. subtilus and S. aureus, two gram-negative bacteria viz., E. coli and
K .pneumoniae through „Cup-plate method‟26
using Streptomycin as standard drug by using DMSO as solvent
and these results were confirmed by an experiment run at a concentration of 40 µg/ml (Table 1). It has been
observed that the compounds exhibited interesting biological activity however, with a degree of variation.
Among all the synthesized compounds, Compound 6c against B. subtilus and S. aureus, compounds 6c, 6d and
6g against S. aureus were determined to be of excellent activity. Compounds 6b, 6d, 6f and 6g against B.
subtilus, compounds 6b and 6f towards S. aureus, the tested compounds 6c and 6d against E. coli and the
compound 6d against K. pneumoniae were exhibited intermediate activity. While the remaining compounds
showed moderate to low activity against all the organisms employed under the conditions of this experiment.
ANTIFUNGAL ACTIVITY
The newly prepared compounds were also screened for growth inhibition against two fungal organisms
namely F. oxysporum and A. niger by using Fluconazole as standard drug with same method and solvent. The
activity of the tested compounds is listed in Table 1. At 40 µg/ml concentration, Compounds 6b, 6d and 6g
showed the greatest biological activity against F. oxysporum since the growth was almost completely inhibited
during the entire incubation period and compounds 6b and 6g are most active against A. niger. Compounds 6c
and 6f showed pronounced growth inhibition against F. oxysporum and compound 6d against A. niger. The
remaining compounds were moderate to less active.
EXPERIMENTAL
All reagents and solvents were used as purchased without further purification. Melting points were
determined on a Fisher–Johns melting point apparatus and are uncorrected. Crude products were purified by
3. Synthesis, Characterization And Biological Evaluation…
www.ijpsi.org 29 | Page
column chromatography on silica gel of 60-120 mesh. IR spectra were obtained on a Perkin Elmer BX serried
FTIR 5000 spectrometer using KBr pellet. NMR spectra were recorded on a Varian 300 MHz spectrometer for
1
H NMR. The chemical shifts were reported as ppm down field using TMS as an internal standard. Mass
spectra were recorded on a VG-Micromass 7070H spectrometer operating at 70 eV.
Synthesis of 2-(α-hydroxy)ethyl benzimidazoles (3a-d)
o-Phenylenediamine (1a-d) (0.01 mol) was treated with lactic acid (2) (0.01 mol) in presence of 4N
hydrochloric acid (5 mL) and refluxed on water both for 24 h. After completion of the reaction (monitored by
TLC), the reaction mixture was cooled and neutralized with NH3 solution to get solid which is separated
through filter and recrystallized from absolute ethanol to afford 3a-d in pure form.
Synthesis of 2-acetyl benzimidazoles (4a-d)
To a solution of 2-(α-hydroxy)ethyl benzimidazole (3a-d) (0.01 mol) in dil.H2SO4 (5%, 40 mL) was drop wise
added the solution of K2Cr2O7 (0.15 mol) and aqueous H2SO4 (25%, 80 mL) with constant stirring at room
temperature over a period of 20 min. Further the reaction mixture was stirred at room temperature for 2 h. After
completion of the reaction, (monitored by TLC), the reaction mixture neutralized with NH3 solution (1:1) and
formed solid was filtered, washed with water and dried, recrystallized from ethyl acetate to achieve 4a-d in pure
form.
Synthesis of 1-(1H-benzimidazol-2-yl)-3-(substituted phenyl) prop-2-en-1-ones (5a-h)
2-Acetyl benzimidazole (4a-d) (0.01 mol) and aromatic benzaldehyde (0.01 mol) were mixed in ethanol (20
mL) and added 60% aq. KOH (5 mL) and the mixture was constantly stirred at room temperature for 4 h. After
completion of reaction (monitored by TLC) the reaction mixture was poured into ice cold water and neutralized
with dil HCl solution to get solid which is recrystallized from ethanol to get 5a-d in pure form.
Synthesis of 2-[(5-aryl)-4,5-dihydro-1H-pyrazole-3-yl]-1H-benzimidazoles (6a-h)
1-(1H-Benzimidazol-2-yl)-3-(substituted phenyl)prop-2-en-1-ones (5a-h) (0.01 mol) and hydrazine hydrate (0.04
mol) was dissolved in glacial acetic acid (10 ml) and refluxed the reaction mixture on water both for 5-6 h. After
completion of reaction (monitored by TLC) the reaction mixture was poured into ice cold water and neutralized with
ammonia solution. The formed solid was filtered, dried and recrystallized from ethyl acetate to obtain compounds
6a-h in pure form.
1-(1H-benzo[d]imidazol-2-yl)-1-ethanol (3a) Yellow solid, yield 90%, mp 180-182 o
C. IR (KBr) cm–1
: 2971,
1623, 1458, 1215, 1103. 1
H NMR (CDCl3) δ: 10.30 (1H, bs), 7.52 (2H, m, J=7.8 Hz), 7.12 (2H, m, J=7.6), 4.8
(1H, s), 3.05 (1H, q, J=7.4 Hz), 1.62 (3H, d, J=7.2 Hz). MS m/z: 163 (M+
+1).
1-(5-methyl-1H-benzo[d]imidazol-2-yl)-1-ethanol (3b) Dark yellow solid, yield 90%, mp 160-162 o
C. IR
(KBr) cm–1
: 3038, 2701, 1629, 1449, 1316, 1101. 1
H NMR (CDCl3) δ: 9.61 (1H, bs), 7.32 (3H, m, J=8.0 Hz),
4.85 (1H, s), 3.05 (1H, q, J=7.8 Hz), 1.62 (3H, d, J=7.4 Hz). MS m/z: 177 (M+
+1).
1-(5-chloro-1H-benzo[d]imidazol-2-yl)-1-ethanol (3c) Brown solid, yield 65%, mp 171-173 o
C. IR (KBr) cm–
1
: 2981, 1623, 1444, 1210, 1082. 1
H NMR (CDCl3) δ: 12.50 (1H, s), 7.55 (2H, d, J=7.2 Hz), 7.20 (1H, d, J=7.4
Hz), 4.91 (1H, m, J=6.8 Hz), 1.52 (3H, d, J=7.0 Hz). MS m/z: 197 (M+
+1).
1-(5-nitro-1H-benzo[d]imidazol-2-yl)-1-ethanol (3d) Brown solid, yield 75%, mp 148-150 o
C. IR (KBr) cm–1
:
3342, 3215, 3024, 2865, 2240, 1420, 1248. 1
H NMR (CDCl3) δ: 8.63 (1H, s), 7.91 (1H, d, J=7.0 Hz), 7.76 (1H,
d, J=7.2 Hz), 6.64 (1H, s), 6.59 (1H, d, J=7.4 Hz), 5.16 (1H, m, J=7.6 Hz), 1.77 (1H, d, J=7.8 Hz). MS m/z:
208 (M+
+1).
1-(1H-benzo[d]imidazol-2-yl)-1-ethanone (4a) Yellow solid, yield 78%, mp 189-191 o
C. IR (KBr) cm–1
:
3289, 3059, 3015, 1674, 1580, 1445, 1235, 1147. 1
H NMR (CDCl3) δ: 13.02 (1H, s), 7.85 (1H, d, J=7.8 Hz),
7.52 (1H, d, J=7.6 Hz), 7.32 (2H, t, J=7.4 Hz), 2.74 (3H, s). MS m/z: 161 (M+
+1).
1-(5-methyl-1H-benzo[d]imidazol-2-yl)-1-ethanone (4b) Yellow solid, yield 80%, mp 170-172 o
C. IR (KBr)
cm–1
: 3365, 2919, 2852, 1693. 1
H NMR (CDCl3) δ: 11.23 (1H, s), 7.65 (1H, d, J=8.0 Hz), 7.48 (1H, d, J=7.8
Hz), 7.24 (1H, s), 3.42 (3H, s), 2.45 (3H, s). MS m/z: 174 (M+
+1).
1-(5-chloro-1H-benzo[d]imidazol-2-yl)-1-ethanone (4c) Yellow solid, yield 65%, mp 185-187 o
C. IR (KBr)
cm–1
: 3294, 3066, 3021, 1677, 1574, 1335, 1219, 1060. 1
H NMR (CDCl3) δ: 10.70 H, s), 7.82 (1H, t, J=7.6 Hz),
7.51 (1H, m, J=7.4 Hz), 7.30 (1H, m, J=7.2 Hz), 2.81 (3H, s). MS m/z: 195 (M+
+1).
1-(5-nitro-1H-benzo[d]imidazol-2-yl)-1-ethanone (4d) Pale yellow solid, yield 70%, mp 155-157 o
C. IR
(KBr) cm–1
: 3360, 3040, 2865, 2160, 1720, 1356, 1240. 1
H NMR (CDCl3) δ: 8.91 (1H, s), 8.77 (1H, s), 8.13
(1H, d, J=7.2 Hz), 8.09 (1H, d, J=7.4 Hz), 2.79 (3H, s). MS m/z: 206 (M+
+1).
(E)-1-(1H-benzo[d]imidazol-2-yl)-3-phenyl-2-propen-1-one (5a) Pale yellow solid, yield 69%, mp 162-164
o
C. IR (KBr) cm–1
: 3276, 2856, 1589, 1487, 1238. 1
H NMR (CDCl3) δ: 8.77 (1H, s), 8.11 (2H, d, J=8.8 Hz),