Benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids: Design,synthesis and in vitro anti-mycobacterial activity evaluation |
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Authors: | Yaohuan Zhang Ruo Wang Tesen Zhang Weitao Yan Yihong Chen Yanping Zhang Muyang Zhou |
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Institution: | College of Chemistry, Fuzhou University, Fuzhou 350116, China |
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Abstract: | 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. |
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Keywords: | Benzofuran Isatin Hybrid compounds Anti-mycobacterial Anti-tubercular Multi-drug resistant Structure-activity relationship |
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