Please use this identifier to cite or link to this item: https://idr.l2.nitk.ac.in/jspui/handle/123456789/12217
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dc.contributor.authorNayak, N.-
dc.contributor.authorRamprasad, J.-
dc.contributor.authorUdayakumar, D.-
dc.date.accessioned2020-03-31T08:38:48Z-
dc.date.available2020-03-31T08:38:48Z-
dc.date.issued2015-
dc.identifier.citationBioorganic and Medicinal Chemistry Letters, 2015, Vol.25, 23, pp.5540-5545en_US
dc.identifier.urihttps://idr.nitk.ac.in/jspui/handle/123456789/12217-
dc.description.abstractWith the aim of developing promising antitubercular and antibacterial leads, we have designed and synthesized a new series of isonicotinohydrazide based pyrazole derivatives (5a-r). All new derivatives (4a-b and 5a-r) were screened for in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv (MTB) strain. Four compounds 5j, 5k, 5l and 4b emerged as promising antitubercular agents with MIC of ?4.9 ?M which is much lower than the MIC of the first line antitubercular drug, ethambutol. The 3-chlorophenyl substituent at position-3 of the pyrazole ring enhanced the antiTB activity of the molecules. Three derivatives 5b, 5k and 4b exhibited promising antibacterial activity against the tested bacterial strains. The active molecules were nontoxic to normal Vero cells and showed high selectivity index (>160). The structure and antitubercular activity relationship was further supported by in silico molecular docking study of the active compounds against enoyl acyl carrier protein reductase (InhA) enzyme of M. tuberculosis. 2015 Published by Elsevier Ltd.en_US
dc.titleNew INH-pyrazole analogs: Design, synthesis and evaluation of antitubercular and antibacterial activityen_US
dc.typeArticleen_US
Appears in Collections:1. Journal Articles

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