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

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 ?M, 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.

SUBMITTER: Lu X

PROVIDER: S-EPMC6071830 | biostudies-other | 2017 Jun

REPOSITORIES: biostudies-other

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

Lu Xiaoyun X Hu Xianglong X Liu Zhiyong Z Zhang Tianyu T Wang Ruibing R Wan Baojie B Franzblau Scott G SG You Qidong Q

MedChemComm 20170428 6

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 ...[more]

PMID: 30108841

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