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:Division of Medicinal Chemistry, Department of Chemistry (DST-FIST Sponsored), Mahatma Gandhi Campus, Maharaja Krishnakumarsinhji Bhavnagar University, Bhavnagar 364 002, Gujarat, India.
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.