A series of new 5-Chloroisatin derivates have been synthesized by the method of N-alkylation at room temperature, in the presence of a base and a catalyst with good yields. The chemical structures of these compounds were confirmed by NMR (1H &13C), these new compounds obtained were evaluated for their antibacterial activity. The final results revealed that the majority of the compounds exhibited good antimicrobial activity against various organisms
Anthranilic acid on heating with a primary amide
resulted in benzamidomethyl/ phthalimidomethyl-quinazolin 4
(3H) ones (II) which on treatment with phosphorus oxychloride
(POCl3) and phosphorus pentachloride (PCl5) afforded 4-chloro-
2-benzamidomethyl/phthalimidomethyl-quinazolines (III).
Reaction of (III) with o-phenylenediamine in anhydrous pyridine
furnished 2-benzamidomethyl/ phthalimido-methylbenzimidazolo
[2, 1-c] quinazolines (IV). A part of synthetic
strategy was also adopted for the synthesis of 2-
benzamidomethyl/ phthalimidomethyl-tetrazolo [1, 5-c]
quinazolines (V) with the interaction of (III) with sodium azide
(NaN3) indimethyl sulphoxide (DMSO) solvent (Scheme)
Synthesis, Characterization, and Antibacterial Activity of Some Novel 5-Chlor...IJERA Editor
The development of potential antibacterial requires the synthesis of a new series of 5- Chloroisatin derivatives incorporating various aromatic aldehydes in the case 1,3-Dipolar Cycloaddition including Nitrile oxide, as well as the cycloaddition Alcyne-Azide Catalytic with Copper. The charcterization of the structure of the synthesized compounds was confirmed by means of their IR, 1H-NMR and 13C-NMR spectral data. In addition, the antibacterial properties in vitro were tested against certain microorganisms using the disk diffusion technique. A majority of compounds show better activity against several of the microorganisms.
Synthesis, characterization and antimicrobial evaluation of novel diethyl (2-...iosrphr_editor
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).
Simple and Eco-friendly Synthesis of Glycosides bearing triazolo[3,4-b][1,3,4...IOSRJAC
There is a vast variety of naturally occurring glycosides which have marked pharmacological properties. These glycosides have widely diversed functional groups modifications which result in influencing pharmacological performance of corresponding glycosides. The 3,6-disubstituted-s-triazolo[3,4- b][1,3,4]thiadiazoles were glucosidated with 2,3,4,6tetra-o-acetyl α D glulopryanosyl bromide using simple methodologies. The compounds obtained in good yield in a 80-90 minutes.
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.
Anthranilic acid on heating with a primary amide
resulted in benzamidomethyl/ phthalimidomethyl-quinazolin 4
(3H) ones (II) which on treatment with phosphorus oxychloride
(POCl3) and phosphorus pentachloride (PCl5) afforded 4-chloro-
2-benzamidomethyl/phthalimidomethyl-quinazolines (III).
Reaction of (III) with o-phenylenediamine in anhydrous pyridine
furnished 2-benzamidomethyl/ phthalimido-methylbenzimidazolo
[2, 1-c] quinazolines (IV). A part of synthetic
strategy was also adopted for the synthesis of 2-
benzamidomethyl/ phthalimidomethyl-tetrazolo [1, 5-c]
quinazolines (V) with the interaction of (III) with sodium azide
(NaN3) indimethyl sulphoxide (DMSO) solvent (Scheme)
Synthesis, Characterization, and Antibacterial Activity of Some Novel 5-Chlor...IJERA Editor
The development of potential antibacterial requires the synthesis of a new series of 5- Chloroisatin derivatives incorporating various aromatic aldehydes in the case 1,3-Dipolar Cycloaddition including Nitrile oxide, as well as the cycloaddition Alcyne-Azide Catalytic with Copper. The charcterization of the structure of the synthesized compounds was confirmed by means of their IR, 1H-NMR and 13C-NMR spectral data. In addition, the antibacterial properties in vitro were tested against certain microorganisms using the disk diffusion technique. A majority of compounds show better activity against several of the microorganisms.
Synthesis, characterization and antimicrobial evaluation of novel diethyl (2-...iosrphr_editor
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).
Simple and Eco-friendly Synthesis of Glycosides bearing triazolo[3,4-b][1,3,4...IOSRJAC
There is a vast variety of naturally occurring glycosides which have marked pharmacological properties. These glycosides have widely diversed functional groups modifications which result in influencing pharmacological performance of corresponding glycosides. The 3,6-disubstituted-s-triazolo[3,4- b][1,3,4]thiadiazoles were glucosidated with 2,3,4,6tetra-o-acetyl α D glulopryanosyl bromide using simple methodologies. The compounds obtained in good yield in a 80-90 minutes.
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.
SYNTHESIS AND CHARACTERIZATION OF SOME TRANSITION METAL COMPLEXES WITH A NEW ...EDITOR IJCRCPS
A new monodentate phosphorus yield Ph3P=CHC(O)C6H4-m-Br (L),was synthesized and characterized with elemental analysis as
well as various spectroscopic techniques. The reactions of the title ylide with mercury(II) halides in equimolar ratios using dry
methanol as solvent have yielded [L.HgX2]2 (X= Cl (1), Br (2), I (3)). The reaction of 1 equiv. this ylide with Cd(NO3)2.4H2O in the
same solvent give a polynuclear complex [Cd (L)(NO3)(μ-NO3)]n (4), followed by treatment with 2 equiv. AgNO3 and AgOTf led to
monomeric chelate complexes 5 and 6, respectively. Characterization of the obtained compounds was also performed by
elemental analysis, IR, 1H, 31P and 13C NMR. All DMSO-solved synthesized compounds were subjected to biological evaluation for
their antibacterial against 6 Gram positive and negative bacteria effects by disc diffusion method. Results showed antibacterial
activity for studied metal complexes and suggested their possible application as antibacterial agents.
Keywords: Phosphorus yields, mercury(II) complexes, silver(I) complexes, cadmium(II) complexes, antibacterial activity.
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.
ANTIMICROBIAL AND ANTIFUNGAL OF SOME NEW SEMISYNTHETIC TERPENOID DERIVATIVES ...Jing Zang
The synthesis of a series of euphorbol derivatives is described, starting from euphorbol isolated from fresh latex of Euphorbia resinifera Berg. Their structures have been established on the basis of spectral data. All compounds were evaluated for antibacterial activities against Escherichia coli and Staphyloccus aureus strains and antifungal activity against Candida albicans and Aspergillus niger strains by using serial dilution method. `
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Journals,
International Journals,
High Impact Journals,
Monthly Journal,
Good quality Journals,
Research,
Research Papers,
Research Article,
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erpublication.org,
Engineering Journal,
Science Journals,
Solvent Extraction Method for the Separation of Cerium(III) as
Cations From Aqueous Media By use 4-[N-(5-methyl isoxazol-3-
yl)benzene sulfonamide azo]-1- Naphthol Coupled With
Spectroscopic Method For Determination
Quality-by-design-based development and validation of a stability-indicating ...Ratnakaram Venkata Nadh
A systematic design-of-experiments was performed by applying quality-by-design concepts to determine
design space for rapid quantification of teriflunomide by the ultraperformance liquid chromatography
(UPLC) method in the presence of degradation products. Response surface and central composite
quadratic were used for statistical evaluation of experimental data using a Design-Expert software. The
response variables such as resolution, retention time, and peak tailing were analyzed statistically for the
screening of suitable chromatographic conditions. During this process, various plots such as perturbation,
contour, 3D, and design space were studied. The method was developed through UPLC BEH C18
2.1 � 100 mm, 1.7-μ column, mobile phase comprised of buffer (5 mM K2HPO4 containing 0.1%
triethylamine, pH 6.8), and acetonitrile (40:60 v/v), the flow rate of 0.5 mL min 1 and UV detection at
250 nm. The method was developed with a short run time of 1 min. Forced degradation studies revealed
that the method was stability-indicating, suitable for both assay and in-vitro dissolution of a drug product.
The method was found to be linear in the range of 28–84 μg mL 1, 2.8–22.7 μg mL 1 with a correlation
coefficient of 0.9999 and 1.000 for assay and dissolution, respectively. The recovery values were found in
the range of 100.1–101.7%. The method was validated according to ICH guidelines.
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.
Synthesis, Anticonvulsant Activity and Cytotoxicity of Novel Valproic Acid De...IOSRJAC
Objective: The aim of this work was to construct novel hydrazones and thiosemsicarbazide derivatives of valproic acid. The new targets will be evaluated for their anticonvulsant activity and cytotoxicity effects. Methods:Targets 7a-k, 10. 11 were synthesized starting from valproic acid using benzotriazole activation and hydrazide and thiosemicarbazide chemistry. The anticonvulsant activity was evaluated by pentylenetetrazoleinduced seizures modes using sodium valproate as a standard for comparison of the activity. The compounds with high anticonvulsant activity were subsequently examined for cytotoxicity against HepG2 by MTT assay. Results:The new targets were characterized using 1HNMR and 13CNMR and their purity were authenticated by elemental analysis. Four compounds 7e, 7j, 10 and 11exhibited the most potent anticonvulsant activity associated with low cytotixicity. Conclusion: Compounds 11 exhibited a moderate anticonvulsant activity and a significantly lower cytotoxicity than valproic acid and 5-fluorouracile suggesting that it could be used as a lead for the development of better anticonvulsant drug candidates.
Synthesis, Molecular Docking and Antimicrobial Evaluation of New Tetrahydrobe...ijtsrd
A series of novel derivatives of Tetrahydrobenzothienopyrimidine hydrazone were synthesized and product structure was elucidated by 1NMR, C13NMR and mass spectroscopy. The synthesized compounds were evaluated against fungal and bacterial strains. The synthesized compounds showed significant antibacterial activity against Staphylococcus aureus MTCC 96, Staphylococcus pyrogenes MTCC 442, and Escherichia coli MTCC 443, Pseudomonas aeruginosa MTCC 1688 and against fungal strains Candida albicans MTCC 227, Aspergillus niger MTCC 282, Aspergillus clavatus MTCC 1323. Some derivatives showed promising result against gram positive, gram negative bacterial and fungal strains than standard drug ampicillin and grieseofulvin. In- silico molecular docking studies of the synthesized compounds was done by using GRIP batch docking method of Vlife MDS 3.0 software to study their observed activity which showed a significant correlation between the binding score and biological activity for synthesized compounds. Neetu Chopra | Kiranpreet kaur | Sanjeev Kumar "Synthesis, Molecular Docking and Antimicrobial Evaluation of New Tetrahydrobenzothienopyrimidine Derivatives" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-2 | Issue-6 , October 2018, URL: http://www.ijtsrd.com/papers/ijtsrd18756.pdf
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.
Photocatalytic Degradation of Ciprofloxacin using TiO2 in a Slurry Photocatal...ijtsrd
A slurry photocatalytic reactor assessed for the degradation of ciprofloxacin CFX . The effect of operating parameters like initial ciprofloxacin concentration, catalyst dosage and pH on ciprofloxacin degradation was analysed in this study. Batch study was conducted and it showed 90 degradation of the CFX. It was observed the optimum concentration of CFX was 1500 µg l, catalyst dosage was 1 g l at the pH of 9 for the duration of 3 hours. The photocatalytic degradation of CFX followed the pseudo first order kinetics. Karthika. V | Vedavalli. S | Afreen Begum. M "Photocatalytic Degradation of Ciprofloxacin using TiO2 in a Slurry Photocatalytic Reactor: Optimization" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-4 | Issue-4 , June 2020, URL: https://www.ijtsrd.com/papers/ijtsrd31224.pdf Paper Url :https://www.ijtsrd.com/engineering/environment-engineering/31224/photocatalytic-degradation-of-ciprofloxacin-using-tio2-in-a-slurry-photocatalytic-reactor-optimization/karthika-v
Adsorption Characteristics and Behaviors of Natural Red Clay for Removal of B...ijtsrd
The present study deals with the analysis and adsorption of Basic Yellow 28 BY28 onto low-cost natural red clay NRC . Adsorbent characterized by XRD, SEM, TG DTA, BET and BJH. The effect of the contact time, the temperature, the initial concentration, the pH and the adsorbent mass and on adsorption process were investigated using by batch adsorption technique and then the adsorption isotherm, kinetics, thermodynamics and equilibrium studies were performed. The pH effect on the removal of BY28 efficiency was not important. It was found that the isotherm model best suited to the equilibrium data obtained from the adsorption of BY28 on NRC was the pseudo-second order. It was found that the kinetic model best suited to the data obtained from the adsorption of BY28 on NRC was the Langmuir model. The maximum monolayer adsorption capacity was 370 mg. g-1. In the thermodynamic studies, it can be said that the adsorption of BY28 onto NRC takes place spontaneously, physically and endothermic ally. Finally, the use of NRC shows a greater potential for the removal of cationic dyes, as no costly equipment is required. Omer Lacin | Ali Haghighatnia | Fatih Demir | Fatih Sevim "Adsorption Characteristics and Behaviors of Natural Red Clay for Removal of BY28 from Aqueous Solutions" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-3 | Issue-2 , February 2019, URL: https://www.ijtsrd.com/papers/ijtsrd21544.pdf
Paper URL: https://www.ijtsrd.com/engineering/engineering-chemistry/21544/adsorption-characteristics-and-behaviors-of-natural-red-clay-for-removal-of-by28-from-aqueous-solutions/omer-lacin
Catalytic Conversion of Biomass using Solid Acid Catalystspbpbms6
The processes for synthesis of several value-added chemicals from biomass (hemicellulose and ignin) using solid acid catalysts are documented in this presentation. Particularly, C5 sugars and furfural are synthesized from hemicellulose and various aromatic monomers are obtained from lignin.
SYNTHESIS AND CHARACTERIZATION OF SOME TRANSITION METAL COMPLEXES WITH A NEW ...EDITOR IJCRCPS
A new monodentate phosphorus yield Ph3P=CHC(O)C6H4-m-Br (L),was synthesized and characterized with elemental analysis as
well as various spectroscopic techniques. The reactions of the title ylide with mercury(II) halides in equimolar ratios using dry
methanol as solvent have yielded [L.HgX2]2 (X= Cl (1), Br (2), I (3)). The reaction of 1 equiv. this ylide with Cd(NO3)2.4H2O in the
same solvent give a polynuclear complex [Cd (L)(NO3)(μ-NO3)]n (4), followed by treatment with 2 equiv. AgNO3 and AgOTf led to
monomeric chelate complexes 5 and 6, respectively. Characterization of the obtained compounds was also performed by
elemental analysis, IR, 1H, 31P and 13C NMR. All DMSO-solved synthesized compounds were subjected to biological evaluation for
their antibacterial against 6 Gram positive and negative bacteria effects by disc diffusion method. Results showed antibacterial
activity for studied metal complexes and suggested their possible application as antibacterial agents.
Keywords: Phosphorus yields, mercury(II) complexes, silver(I) complexes, cadmium(II) complexes, antibacterial activity.
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.
ANTIMICROBIAL AND ANTIFUNGAL OF SOME NEW SEMISYNTHETIC TERPENOID DERIVATIVES ...Jing Zang
The synthesis of a series of euphorbol derivatives is described, starting from euphorbol isolated from fresh latex of Euphorbia resinifera Berg. Their structures have been established on the basis of spectral data. All compounds were evaluated for antibacterial activities against Escherichia coli and Staphyloccus aureus strains and antifungal activity against Candida albicans and Aspergillus niger strains by using serial dilution method. `
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,
Solvent Extraction Method for the Separation of Cerium(III) as
Cations From Aqueous Media By use 4-[N-(5-methyl isoxazol-3-
yl)benzene sulfonamide azo]-1- Naphthol Coupled With
Spectroscopic Method For Determination
Quality-by-design-based development and validation of a stability-indicating ...Ratnakaram Venkata Nadh
A systematic design-of-experiments was performed by applying quality-by-design concepts to determine
design space for rapid quantification of teriflunomide by the ultraperformance liquid chromatography
(UPLC) method in the presence of degradation products. Response surface and central composite
quadratic were used for statistical evaluation of experimental data using a Design-Expert software. The
response variables such as resolution, retention time, and peak tailing were analyzed statistically for the
screening of suitable chromatographic conditions. During this process, various plots such as perturbation,
contour, 3D, and design space were studied. The method was developed through UPLC BEH C18
2.1 � 100 mm, 1.7-μ column, mobile phase comprised of buffer (5 mM K2HPO4 containing 0.1%
triethylamine, pH 6.8), and acetonitrile (40:60 v/v), the flow rate of 0.5 mL min 1 and UV detection at
250 nm. The method was developed with a short run time of 1 min. Forced degradation studies revealed
that the method was stability-indicating, suitable for both assay and in-vitro dissolution of a drug product.
The method was found to be linear in the range of 28–84 μg mL 1, 2.8–22.7 μg mL 1 with a correlation
coefficient of 0.9999 and 1.000 for assay and dissolution, respectively. The recovery values were found in
the range of 100.1–101.7%. The method was validated according to ICH guidelines.
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.
Synthesis, Anticonvulsant Activity and Cytotoxicity of Novel Valproic Acid De...IOSRJAC
Objective: The aim of this work was to construct novel hydrazones and thiosemsicarbazide derivatives of valproic acid. The new targets will be evaluated for their anticonvulsant activity and cytotoxicity effects. Methods:Targets 7a-k, 10. 11 were synthesized starting from valproic acid using benzotriazole activation and hydrazide and thiosemicarbazide chemistry. The anticonvulsant activity was evaluated by pentylenetetrazoleinduced seizures modes using sodium valproate as a standard for comparison of the activity. The compounds with high anticonvulsant activity were subsequently examined for cytotoxicity against HepG2 by MTT assay. Results:The new targets were characterized using 1HNMR and 13CNMR and their purity were authenticated by elemental analysis. Four compounds 7e, 7j, 10 and 11exhibited the most potent anticonvulsant activity associated with low cytotixicity. Conclusion: Compounds 11 exhibited a moderate anticonvulsant activity and a significantly lower cytotoxicity than valproic acid and 5-fluorouracile suggesting that it could be used as a lead for the development of better anticonvulsant drug candidates.
Synthesis, Molecular Docking and Antimicrobial Evaluation of New Tetrahydrobe...ijtsrd
A series of novel derivatives of Tetrahydrobenzothienopyrimidine hydrazone were synthesized and product structure was elucidated by 1NMR, C13NMR and mass spectroscopy. The synthesized compounds were evaluated against fungal and bacterial strains. The synthesized compounds showed significant antibacterial activity against Staphylococcus aureus MTCC 96, Staphylococcus pyrogenes MTCC 442, and Escherichia coli MTCC 443, Pseudomonas aeruginosa MTCC 1688 and against fungal strains Candida albicans MTCC 227, Aspergillus niger MTCC 282, Aspergillus clavatus MTCC 1323. Some derivatives showed promising result against gram positive, gram negative bacterial and fungal strains than standard drug ampicillin and grieseofulvin. In- silico molecular docking studies of the synthesized compounds was done by using GRIP batch docking method of Vlife MDS 3.0 software to study their observed activity which showed a significant correlation between the binding score and biological activity for synthesized compounds. Neetu Chopra | Kiranpreet kaur | Sanjeev Kumar "Synthesis, Molecular Docking and Antimicrobial Evaluation of New Tetrahydrobenzothienopyrimidine Derivatives" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-2 | Issue-6 , October 2018, URL: http://www.ijtsrd.com/papers/ijtsrd18756.pdf
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.
Photocatalytic Degradation of Ciprofloxacin using TiO2 in a Slurry Photocatal...ijtsrd
A slurry photocatalytic reactor assessed for the degradation of ciprofloxacin CFX . The effect of operating parameters like initial ciprofloxacin concentration, catalyst dosage and pH on ciprofloxacin degradation was analysed in this study. Batch study was conducted and it showed 90 degradation of the CFX. It was observed the optimum concentration of CFX was 1500 µg l, catalyst dosage was 1 g l at the pH of 9 for the duration of 3 hours. The photocatalytic degradation of CFX followed the pseudo first order kinetics. Karthika. V | Vedavalli. S | Afreen Begum. M "Photocatalytic Degradation of Ciprofloxacin using TiO2 in a Slurry Photocatalytic Reactor: Optimization" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-4 | Issue-4 , June 2020, URL: https://www.ijtsrd.com/papers/ijtsrd31224.pdf Paper Url :https://www.ijtsrd.com/engineering/environment-engineering/31224/photocatalytic-degradation-of-ciprofloxacin-using-tio2-in-a-slurry-photocatalytic-reactor-optimization/karthika-v
Adsorption Characteristics and Behaviors of Natural Red Clay for Removal of B...ijtsrd
The present study deals with the analysis and adsorption of Basic Yellow 28 BY28 onto low-cost natural red clay NRC . Adsorbent characterized by XRD, SEM, TG DTA, BET and BJH. The effect of the contact time, the temperature, the initial concentration, the pH and the adsorbent mass and on adsorption process were investigated using by batch adsorption technique and then the adsorption isotherm, kinetics, thermodynamics and equilibrium studies were performed. The pH effect on the removal of BY28 efficiency was not important. It was found that the isotherm model best suited to the equilibrium data obtained from the adsorption of BY28 on NRC was the pseudo-second order. It was found that the kinetic model best suited to the data obtained from the adsorption of BY28 on NRC was the Langmuir model. The maximum monolayer adsorption capacity was 370 mg. g-1. In the thermodynamic studies, it can be said that the adsorption of BY28 onto NRC takes place spontaneously, physically and endothermic ally. Finally, the use of NRC shows a greater potential for the removal of cationic dyes, as no costly equipment is required. Omer Lacin | Ali Haghighatnia | Fatih Demir | Fatih Sevim "Adsorption Characteristics and Behaviors of Natural Red Clay for Removal of BY28 from Aqueous Solutions" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-3 | Issue-2 , February 2019, URL: https://www.ijtsrd.com/papers/ijtsrd21544.pdf
Paper URL: https://www.ijtsrd.com/engineering/engineering-chemistry/21544/adsorption-characteristics-and-behaviors-of-natural-red-clay-for-removal-of-by28-from-aqueous-solutions/omer-lacin
Catalytic Conversion of Biomass using Solid Acid Catalystspbpbms6
The processes for synthesis of several value-added chemicals from biomass (hemicellulose and ignin) using solid acid catalysts are documented in this presentation. Particularly, C5 sugars and furfural are synthesized from hemicellulose and various aromatic monomers are obtained from lignin.
Synthesis of 1,2,3-Triazole 5-Chloroisatin Derivatives via Copper-Catalyzed 1...IJAEMSJORNAL
A facile and simple protocol for the ‘Click’ cycloaddition of organic azides with N-propargylchloroisatine catalyzed by CuI, produces in good yields novel of 1,4-disubstituted 1,2,3-triazoles were obtained. Compared to the uncatalyzed cycloaddition, the yields are significantly improved in the presence of CuI as catalyst, without alteration of the selectivity. The regio- and stereochemistry of the cycloadducts has been corroborated by 1H, 13C NMR spectroscopy.
Detailed characterization of saponins isolated from Zygophyllum Propinqueem D...Open Access Research Paper
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Indigenized remote control interface card suitable for MAFI system CCR equipment. Compatible for IDM8000 CCR. Backplane mounted serial and TCP/Ethernet communication module for CCR remote access. IDM 8000 CCR remote control on serial and TCP protocol.
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Indigenized remote control interface card suitable for MAFI system CCR equipment. Compatible for IDM8000 CCR. Backplane mounted serial and TCP/Ethernet communication module for CCR remote access. IDM 8000 CCR remote control on serial and TCP protocol.
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N-alkylation methods, Characterization and Evaluation of antibacterial activity of some Novel 5-Chloroisatin Derivatives
1. Z. Tribak.et.al. Int. Journal of Engineering Research and Application www.ijera.com
ISSN : 2248-9622, Vol. 7, Issue 6, ( Part -5) June 2017, pp.21-24
www.ijera.com DOI: 10.9790/9622-0706052124 21 | P a g e
N-alkylation methods, Characterization and Evaluation of
antibacterial activity of some Novel 5-Chloroisatin Derivatives
Z. Tribak1
, O. El Amin2
, M.K. Skalli1*
, O. Senhaji3
, Y. Kandri. Rodi4
,
M. Houssaini. Iraqui2
1
Laboratory of Applied Chemistry, Sidi Mohamed Ben Abdellah University, Faculty of Sciences and Technology
of Fes, Morocco
2
Laboratory of Microbial Biotechnology, Faculty of Science and Technology, B.P. 2202, Fes, Morocco
3
Laboratory of Applied Physical Chemistry, Moulay Ismaïl University, Faculty of Sciences and Technology of
Errachidia, Morocco.
4
Laboratory of Applied Organic Chemistry, Sidi Mohamed Ben Abdellah University, Faculty of Science and
Technology of Fes, Morocco.
ABSTRACT:
A series of new 5-Chloroisatin derivates have been synthesized by the method of N-alkylation at room
temperature, in the presence of a base and a catalyst with good yields. The chemical structures of these
compounds were confirmed by NMR (1
H &13
C), these new compounds obtained were evaluated for their
antibacterial activity. The final results revealed that the majority of the compounds exhibited good antimicrobial
activity against various organisms.
Keywords: 5-Chloroisatin derivates, N-alkylation, antibacterial activity, NMR
I. INTRODUCTION
The design, synthesis and production of
molecules, are ones of the important objectives of
organic and medicinal chemistry [1], which are
having highly therapeutic interest. Since the
discovery of heterocyclic nucleus the chemistry of
isatin and their fused derivatives has a wide varity of
pharmacological activities such as antimicrobial,
anticancer, antiviral, anticonvulsant, anti-
inflammatory and analgesic [2]. Different research
group attempted study on isatin synthetic aspect.
Otherresearch group attempted study of isatin
biological activity [3].
Thus the structural modification of the
isatin derivates moiety is still of the highest
importance. This article has focused on the
application of synthetic N-alkylation methods in the
conditions of charge transfer catalysis in the
presence of a base (K2CO3) and a catalyst (BTBA)
between 5-Chloro-1H-indole-2,3-dione and
alkylating agents with good to excellent yields [4].
The synthesized 5-Chloroisatin derivatives were
characterized by spectroscopic techniques, such as,
1
H NMR, 13
C NMR. In addition, they were evaluated
for their biological activities [5] as antibacterial in
vitro against two Gram positive bacteria such as
Staphylococcus aureus, Bacillus cereus and two
Gram negative bacteria such as Escherichia coli,
pseudomonas aeruginosa.
II. MATERIAL AND METHODS
1. Chemistry:
All melting points were measured by the
Kofler bench. The 1
H NMR, 13
C NMR spectra were
recorded on Bruker 300 NMR spectrometer
advancement in CDCl3 using tetramethylsilane
(TMS) as reference. Chemical shifts are reported in
parts per million. Reactions were monitored by thin
layer chromatography (TLC) on silica gel, plates
were visualizing with ultraviolet light or iodine.
Column chromatography was performed on silica
gel 60 (0.043-0.06mm) Merck.5-Chloroisatin
derivatives were synthesized by alkylation method
available in the phase transfer catalysis conditions [6,
7]. The synthetic strategies adopted to obtain target
compounds are depicted in Figure 1 and 2.
1.1 GENERAL PROCEDURE FOR THE
SYNTHESIS OF NEW 5-CHLOROISATIN
DERIVATES:
Compounds were then reacted with various
alkylating agent, so into a 100 mL two-necked flask
we introduce 0.2 g (1.1 mmol) of 5-chloro-1H-
indole-2,3-dione (0.23 g, 1.16 mmol) of potassium
carbonate in 15 ml of N-N-dimethylformamide
(DMF) and (0.035 g, 0.10 mmol) of BTBA with
magnetic stirring, the alkylating agent is added
slowly, the mixture is left at room temperature for 48
hours. During this period the progress of the reaction
is monitored by TLC (thin layer chromatography).
Once the reaction is complete, the salts are removed
RESEARCH ARTICLE OPEN ACCESS
3. Z. Tribak.et.al. Int. Journal of Engineering Research and Application www.ijera.com
ISSN : 2248-9622, Vol. 7, Issue 6, ( Part -5) June 2017, pp.21-24
www.ijera.com DOI: 10.9790/9622-0706052124 23 | P a g e
=9Hz); 1.60-1.70 (m, 2H, CH2); 1.22 (s, 22H, CH2),
0.85 (t, 3H, CH3, 3
JH-H =6Hz). 13
C NMR (CDCl3;
75MHz) : δ(ppm) 182.24 (C=O); 161.85 (N-C=O);
137.62, 125.35, 111.41(Cq) ; 130.45, 129.43, 118.46
(CHAr); 40.48, 31.94, 29.65, 29.62, 29.61, 29.54,
29.46, 29.36, 29.21, 27.20, 26.88, 22.70 (CH2);
14.12 (CH3).
Compound 8: 1-(6-bromohexyl)-5-
chloroindoline-2,3-dione:Yield: 85 % ; m.p: 66-
70 °C ; Rf = 0.8 (Hexane/EtOAc, 2:1); 1
H NMR
(CDCl3; 300MHz): δ (ppm) 7.49-7.51 (dd, H,
CHArom ,J4
H-H = 1.5 Hz, J3
H-H = 4.5 Hz) ; 7.47 (d, H,
CHAr ,J4
H-H = 1.5 Hz) ; 6.77 (d, H, CHArom,J3
H-H = 6
Hz) ; 3.65 (t, 2H, CH2, J4
H-H = 3Hz) ; 3.33 (t, 2H,
CH2 , J3
H-H = 6Hz) ; 1.75-1.82 (m, 2H, CH2), 1.61-
1.68 (m, 2H, CH2) , 1.47 (m, 4H, CH2). 13
C NMR
(CDCl3; 75MHz): δ (ppm): 182.64 (C=O); 160.28
(N-C=O); 146.49, 132.61, 119.49 (Cq) ; 134.44,
130.93, 123.33 (CHAr) ; 40.51 , 33.70 , 32.01, 27.89,
27.07, 26.15 (CH2) .
II. IN VITRO ANTIBACTERIAL
ACTIVITY EVALUATION
2.1 A disc diffusion test:
This method makes it possible to evaluate
the antibacterial activity of a product. Although it is
recognized as reliable and reproducible, it is mostly
used as a preliminary stage for further studies as it
provides access to essentially qualitative results. The
technique used is a modification of the method of
Hayes and Markovic.
It consists of depositing a sterile disk
imbibed by the test product on a bacterial mat at the
very beginning of its growth and measuring the area
where the bacteria could not develop. The inhibition
diameter, which reflects the antibacterial activity of
the product tested, is thus determined. The
antimicrobial activity of 5-Chloro-1H-indole-2,3-
dione derivatives was evaluated using the disc
diffusion method [8] using different microorganisms,
including three types of bacteria: Bacillus cereus,
Staphylococcus aureus, Escherichia coli and
Pseudomonas aeruginosa. Mueller Hinton agar
medium (MHA) was used for bacteria. Plates were
preincubated at 37 ° C for 24 h.
A sterile paper disk (6 mm in diameter) was placed
on the surface of each agar plate and impregnated
with 5 μL of each solution of 5-chloroisatin
derivatives at a final concentration of 10 mg / ml.
Then, the Petri dishes are incubated at 37 °C for 24
h for the bacteria. The diameters of the inhibition
zones were measured in mm (including the diameter
of the disk) with the caliper. A disc impregnated
with 2% dimethylsulfoxide as a negative control
was made. Each experiment was carried out in
triplicate.
2.2 MINIMUM INHIBITORY
CONCENTRATION DETERMINATION (MIC):
The minimal inhibitory concentration
(MIC) of our products was evaluated according to
the microdilution method with some modifications.
The minimum inhibitory concentration (MIC) was
determined as the lowest concentration with no
microbial growth compared to the positive control.
DMSO (2%) was used as a negative control.
Briefly, the dilution of the 5-chloroisatin derivatives
was prepared in a Mueller Hinton broth
supplemented with bacteriological agar, to reach a
final concentration between 5 mg / ml and 0.004 mg
/ ml, 50 μL of bacterial inoculum was added to each
well at a final concentration of 106 CFU / ml.
The final concentration of our product was between
5 mg ml-1 (3rd well) and 0.019 mg ml-1 (well 11).
Plates were incubated at 37°C for 24 h. After 2
hours of a subsequent incubation, bacterial growth
was revealed by reduction of blue dye resazurin to
pink resorufin [9].
2.3 MINIMUM BACTERICIDAL
CONCENTRATIONS (MBC):
order to determine the CMB, a bactericidal
control is carried out 24 hours earlier by streaking
on a platelet agar, after microdilution to the broth by
spreading 5 μl of the negative wells on Luria Bertani
agar plates (Luria Bertani medium: Yeast extract 5.0
g, peptone 10.0 g, sodium chloride 5.0 g, distilled
water 1000 ml). The MBC will be the lowest
concentration whose transplant shows a growth of
germ less than or equal to 0.01% of survivors [10].
III. RESULTS AND DISCUSSION :
Table 1: MICs and MBCs of the compounds against the microbes used
compounds
MIC/MBC (mg/mL)
Gram+ Gram-
Bacillus cereus Staphylococcus
aureus
Escherichia coli Pseudomonas
aeruginosa
2 0,156/0,156 0,313/0,313 - -
3 0,078/0,078 0,156/0,156 - -
4 0,078/0,078 0,01/0,01 - -
5 0,625/0,625 0,313/0,313 - -
4. Z. Tribak.et.al. Int. Journal of Engineering Research and Application www.ijera.com
ISSN : 2248-9622, Vol. 7, Issue 6, ( Part -5) June 2017, pp.21-24
www.ijera.com DOI: 10.9790/9622-0706052124 24 | P a g e
6 - - - -
7 - - - -
8 - 1,25/1,25 1,25/1,25
This table showed that compound 4
exercised an excellent inhibitory activity against
Staphylococcus aureus à Gram positive bacteria,
with a MIC value of 0,01 mg/mL, while compounds
3 and 4 displayed comparable activity against
Bacillus cereus with a MIC value of 0,078 mg/ml,
while compounds 3 and 5 displayed moderate to
good activity against Gram positive bacteria studied.
The compounds 8 exhibited moderate inhibitory
effect against Gram+ and Gram- bacteria
(staphylococcus aureus and Escherichia coli) at a
MIC value of 1,25 mg/mL. However, Pseudomonas
aeruginosa (à Gram – bacteria) was resistant to
alltested compounds. Moreover, the compounds 6
and 7 did not show any antimicrobial effects against
all tested strains. Generally, Gram-positive bacteria
are much more susceptible to antibacterial agents
than Gram negative bacteria, whose resistance is
attributed to the structures of their cell wall. Gram-
negative bacteria have a thick lipid bilayer which is
selectively permeable [11].
IV. CONCLUSION
The synthesis of a variety of the 5-
Chloroisatin derivatives was carried out via the N-
alkylation reaction. All compounds were obtained in
good yields. The structures of compounds obtained
were confirmed by 1
H-NMR, 13
C-NMR. The
antimicrobial activity of these compounds was
tested against two Gram-negative bacteria and two
Gram-positive bacteria. From the above results it
can be concluded that, the highest activity was
obtained with the 4 compound which exhibited good
to high activity towards Staphylococcus aureus -
Gram positive bacteria, with a MIC value of 0.01
mg / ml. Compounds 2, 3, 5, 8 showed moderate
activity against the Gram positive bacteria studied,
whereas compounds 6 and 7 showed no
antimicrobial effect.
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