Benzylsulfanyl benzo-heterocycle amides and hydrazones as new agents against drug-susceptible and resistant Mycobacterium tuberculosis123. Issue 6 (18th May 2017)

• Record Type: Journal Article
• Authors: Lu, Xiaoyun; Hu, Xianglong; Liu, Zhiyong; Zhang, Tianyu; Wang, Ruibing; Wan, Baojie; Franzblau, Scott G.; You, Qidong
• Is Part Of: MedChemComm. Volume 8:Issue 6(2017)
• Page Start: 1303
• Page End: 1306
• Publication Date: 2017-05-18
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19
• DOI: 10.1039/c7md00146k
• Languages: English
• ISSNs: 2040-2503

Abstract

Abstract : A series of benzylsulfanyl benzo-heterocycle amides and hydrazones were synthesized and evaluated for anti-tubercular activities. Abstract : A series of benzylsulfanyl benzo-heterocycle amides and hydrazones were synthesized and evaluated for anti-tubercular activities. The isonicotinyl hydrazone derivatives12d, 12e and12f exhibited good anti-tubercular activity against Mycobacterium tuberculosis H37 Rv (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, compound12e 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.