| Literature DB >> 25462270 |
Gilish Jose1, T H Suresha Kumara2, Gopalpur Nagendrappa1, H B V Sowmya1, Dharmarajan Sriram3, Perumal Yogeeswari3, Jonnalagadda Padma Sridevi3, Tayur N Guru Row4, Amar A Hosamani4, P S Sujan Ganapathy5, N Chandrika1, L V Narendra1.
Abstract
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, (1)H NMR, (13)C 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.Entities:
Keywords: Anti-mycobacterial activity; Imidazopyridine amide; InhA; Tuberculosis; X-ray crystallography
Mesh：
Substances：
Year: 2014 PMID： 25462270 DOI： 10.1016/j.ejmech.2014.10.079
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514