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  • Title: Synthesis, molecular docking and anti-mycobacterial evaluation of new imidazo[1,2-a]pyridine-2-carboxamide derivatives.
    Author: Jose G, Suresha Kumara TH, Nagendrappa G, Sowmya HB, Sriram D, Yogeeswari P, Sridevi JP, Guru Row TN, Hosamani AA, Sujan Ganapathy PS, Chandrika N, Narendra LV.
    Journal: Eur J Med Chem; 2015 Jan 07; 89():616-27. PubMed ID: 25462270.
    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.
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