Citation: Zhang Yaohuan, Wang Ruo, Zhang Tesen, Yan Weitao, Chen Yihong, Zhang Yanping, Zhou Muyang. Benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids: Design, synthesis and in vitro anti-mycobacterial activity evaluation[J]. Chinese Chemical Letters, ;2019, 30(3): 653-655. doi: 10.1016/j.cclet.2018.11.032 shu

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

College of Chemistry, Fuzhou University, Fuzhou 350116, China

wangruo1201@gmail.com

Received Date: 9 November 2018
Revised Date: 29 November 2018
Accepted Date: 30 November 2018
Available Online: 30 March 2018

Figures(3)

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 H₃₇Rv 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 H₃₇Rv and MDR-TB isolates, respectively. The results demonstrated the potential utility of benzofuran-isatin-hydroxylimine/-thiosemicarbazide hybrids as anti-TB agents.
- Benzofuran,
- Isatin,
- Hybrid compounds,
- Anti-mycobacterial,
- Anti-tubercular,
- Multi-drug resistant,
- Structure-activity relationship
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沈阳化工大学材料科学与工程学院沈阳 110142