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Benzylsulfanyl benzo-heterocycle amides and hydrazones as new agents against drug-susceptible and resistant Mycobacterium tuberculosis

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Abstract

A series of benzylsulfanyl benzo-heterocycle amides and hydrazones were synthesized and evaluated for anti-tubercular activities. The isonicotinyl hydrazone derivatives 12d, 12e and 12f exhibited good anti-tubercular activity against Mycobacterium tuberculosis H37Rv (ATCC #27294) with MIC values of 0.23, 0.24 and 0.24 μM, respectively, and were also active against SDR-TB, MDR-TB and XDR-TB. More importantly, compound 12e also showed low cytotoxicity and good metabolic stability, and could significantly reduce the mycobacterial burden in a mouse model infected with autoluminescent H37Ra strain, which may serve as a lead compound for further development.

Graphical abstract: Benzylsulfanyl benzo-heterocycle amides and hydrazones as new agents against drug-susceptible and resistant Mycobacterium tuberculosis

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Publication details

The article was received on 24 Mar 2017, accepted on 28 Apr 2017 and first published on 28 Apr 2017


Article type: Research Article
DOI: 10.1039/C7MD00146K
Citation: Med. Chem. Commun., 2017, Advance Article
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    Benzylsulfanyl benzo-heterocycle amides and hydrazones as new agents against drug-susceptible and resistant Mycobacterium tuberculosis

    X. Lu, X. Hu, Z. Liu, T. Zhang, R. Wang, B. Wan, S. G. Franzblau and Q. You, Med. Chem. Commun., 2017, Advance Article , DOI: 10.1039/C7MD00146K

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