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Benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids:Design,synthesis and in vitro anti-mycobacterial activity evaluation

Benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids:Design,synthesis and in vitro anti-mycobacterial activity evaluation

作     者:Yaohuan Zhang Ruo Wang Tesen Zhang Weitao Yan Yihong Chen Yanping Zhang Muyang Zhou 

作者机构:College of Chemistry Fuzhou University Fuzhou 350116 China 

出 版 物:《Chinese Chemical Letters》 (中国化学快报(英文版))

年 卷 期:2019年第30卷第3期

页      码:653-655页

摘      要:A series of novel benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids were designed, synthesized and evaluated for their in vitro anti-TB activities against drug-sensitive MTB H_(37)Rv and MDR-TB isolates as well as cytotoxicity. All benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids exhibited considerable in vitro anti-mycobacterial activities against the tested three MTB strains, and all of them also showed acceptable cytotoxicity. The most active hybrid 7f was >4.8 and >51 folds more potent than the first line anti-TB agents RIF and INH against both drug-sensitive MTB H_(37)Rv and MDR-TB isolates, respectively. The results demonstrated the potential utility of benzofuran-isatin-hydroxylimine/-thiosemicarbazide hybrids as anti-TB agents.

主 题 词:Benzofuran Isatin Hybrid compounds Anti-mycobacterial Anti-tubercular Multi-drug resistant Structure-activity relationship 

学科分类:07[理学] 0703[理学-化学类] 

核心收录:

D O I:10.1016/j.cclet.2018.11.032

馆 藏 号:203455630...

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