Abstract
A novel series of 4-(arylideneamino)-N'-((2-chloro-8-methylquinolin-3-yl)methylene)-3-phenyl-2-thioxo-2,3- dihydrothiazole-5-carbohydrazides (5a-o) bearing biologically active 2-chloroquinoline-3-carbaldehyde and 2-thioxothiazole ring have been synthesized. The structures of synthesized compounds were established by spectroscopic techniques (IR, 1H NMR, 13C NMR and mass spectrometry). Antimicrobial screening of compounds (5a-o) was done against Gram-positive bacteria (Staphylococcus aureus and Streptococcus pyogenes), Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa) and fungi (Candida albicans, Aspergillus niger and Aspergillus clavatus) using serial broth dilution method. SAR for the series was developed by comparing their MIC values with ampicillin and griseofulvin. Some of the compounds from the series like 5o were found to be most active at MIC 12.5 µg/mL against P. Aeruginosa, and compound 5k was found to be most active at MIC 12.5 µg/mL against A. clavatus.
Keywords: Quinoline, 2-Thioxothiazole, Antimicrobial activity.
Letters in Drug Design & Discovery
Title:Synthesis of Some Novel 4-(Arylideneamino)-N'-((2-chloro-8-methylquinolin- 3-yl)methylene)-3-phenyl-2-thioxo-2,3-dihydrothiazole-5-carbohydrazides as Potential Antimicrobial Agents
Volume: 10 Issue: 7
Author(s): N. C. Desai, N R Shihory and G. M. Kotadiya
Affiliation:
Keywords: Quinoline, 2-Thioxothiazole, Antimicrobial activity.
Abstract: A novel series of 4-(arylideneamino)-N'-((2-chloro-8-methylquinolin-3-yl)methylene)-3-phenyl-2-thioxo-2,3- dihydrothiazole-5-carbohydrazides (5a-o) bearing biologically active 2-chloroquinoline-3-carbaldehyde and 2-thioxothiazole ring have been synthesized. The structures of synthesized compounds were established by spectroscopic techniques (IR, 1H NMR, 13C NMR and mass spectrometry). Antimicrobial screening of compounds (5a-o) was done against Gram-positive bacteria (Staphylococcus aureus and Streptococcus pyogenes), Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa) and fungi (Candida albicans, Aspergillus niger and Aspergillus clavatus) using serial broth dilution method. SAR for the series was developed by comparing their MIC values with ampicillin and griseofulvin. Some of the compounds from the series like 5o were found to be most active at MIC 12.5 µg/mL against P. Aeruginosa, and compound 5k was found to be most active at MIC 12.5 µg/mL against A. clavatus.
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Desai C. N., Shihory R N and Kotadiya M. G., Synthesis of Some Novel 4-(Arylideneamino)-N'-((2-chloro-8-methylquinolin- 3-yl)methylene)-3-phenyl-2-thioxo-2,3-dihydrothiazole-5-carbohydrazides as Potential Antimicrobial Agents, Letters in Drug Design & Discovery 2013; 10 (7) . https://dx.doi.org/10.2174/1570180811310070011
DOI https://dx.doi.org/10.2174/1570180811310070011 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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