Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 89, Issue -, Pages 616-627Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.10.079
Keywords
Anti-mycobacterial activity; Imidazopyridine amide; InhA; Tuberculosis; X-ray crystallography
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Funding
- Jain University
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New anti-tubercular agents, imidazo[1,2-a]pyridine-2-carboxamide derivatives (5a-q) have been designed and synthesized. The structural considerations of the designed molecules were further supported by the docking study with a long-chain enoyl-acyl carrier protein reductase (InhA). The chemical structures of the new compounds were characterized by IR, H-1 NMR, C-13 NMR, HRMS and elemental analysis. In addition, single crystal X-ray diffraction has also been recorded for compound 5f. Compounds were evaluated in vitro against Mycobacterium tuberculosis H37Rv, and cytotoxicity against HEK-293T cell line. Amongst the tested compounds 5j, 5l and 5q were emerged as good anti-tubercular agents with low cytotoxicity. The structure-anti TB activity relationship of these derivatives was explained by molecular docking. (C) 2014 Elsevier Masson SAS. All rights reserved.
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