Design, synthesis and in vitro anti-mycobacterial activities of homonuclear and heteronuclear bis-isatin derivatives

被引：26

作者：

Xu, Yan ^{[1
]}

Guan, Jianguo ^{[1
]}

Xu, Zhi ^{[2
]}

Zhao, Shijia ^{[2
]}

机构：

[1] Wuhan Univ Technol, State Key Lab Adv Technol Mat Synth & Proc, Wuhan, Hubei, Peoples R China

[2] Wuhan Univ Sci & Technol, Key Lab Hubei Prov Coal Convers & New Carbon Mat, Wuhan, Hubei, Peoples R China

来源：

FITOTERAPIA | 2018年 / 127卷

关键词：

Isatin; Homonuclear; Heteronuclear; Dimer; Anti-mycobacterial; Structure-activity relationship; ANTI-TUBERCULAR ACTIVITY; ANTIMYCOBACTERIAL EVALUATION; HYBRIDS; CIPROFLOXACIN; AGENTS;

D O I：

10.1016/j.fitote.2018.03.018

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel homonuclear and heteronuclear bis-isatin derivatives tethered through ethylene were designed, synthesized and evaluated for their in vitro anti-mycobacterial activities against MTB H37Rv and MDR-TB. All hybrids exhibited potential anti-mycobacterial activities against MTB H37Rv and MDR-TB with MIC ranging from 16 to 256 mu g/mL. In particular, the heteronuclear bis-isatin 4i (MIC: 25 and 16 mu g/mL) was most active against MTB H37Rv and MDR-TB strains, and could act as a lead for further optimization.

引用

页码：383 / 386

页数：4

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