N. Nayak, J. Ramprasad, U. Dalimba
Mar 1, 2016
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Influential Citations
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Quality indicators
Journal
Chinese Chemical Letters
Abstract
Abstract This article demonstrates the synthesis, characterization and the study of in vitro antitubercular activities of twenty four new N -(4-(5-aryl-3-(5-methyl-1,3,4-oxadiazol-2-yl)-1 H -pyrazol-1-yl)phenyl)-4-amide derivatives ( 8a–x ). The antitubercular activity of the compounds against Mycobacterium tuberculosis H 37 Rv (MTB) revealed that 2-chloro- N -(4-(5-(4-chlorophenyl)-3-(5-methyl-1,3,4-oxadiazol-2-yl)-1 H -pyrazol-1-yl)phenyl)benzamide ( 8n ) is the most promising lead molecule with a MIC of 1.56 μg/mL, while the corresponding unsubstituted benzamide derivative ( 8o ) is the next most active molecule with a MIC of 3.13 μg/mL. Interestingly, the pyrazole intermediate 5b containing chlorophenyl and N -acylcarbohydrazide substituents also showed significant activity (MIC = 3.13 μg/mL). Further, the active molecules did not show toxicity against a normal NIH 3T3 cell line, signifying their suitability for further drug development.