Synthesis and in vitro antimycobacterial activity of 8-OCH3 ciprofloxacin methylene and ethylene isatin derivatives

被引：117

作者：

Feng, Lian-Shun ^{[1
,2
]}

Liu, Ming-Liang ^{[1
,2
]}

Zhang, Shu ^{[3
]}

Chai, Yun ^{[1
,2
]}

Wang, Bo ^{[1
,2
]}

Zhang, Yi-Bin ^{[1
,2
]}

Lv, Kai ^{[1
,2
]}

Guan, Yan ^{[1
,2
]}

Guo, Hui-Yuan ^{[1
,2
]}

Xiao, Chun-Ling ^{[1
,2
]}

机构：

[1] Chinese Acad Med Sci, Inst Med Biotechnol, Beijing 100050, Peoples R China

[2] Peking Union Med Coll, Beijing 100050, Peoples R China

[3] Beijing Univ Technol, Coll Environm & Energy Engn, Dept Chem & Chem Engn, Beijing 100124, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 01期

关键词：

8-OCH3 ciprofloxacin derivatives; Synthesis; Antimycobacterial activity; MYCOBACTERIUM-TUBERCULOSIS; ANTIBACTERIAL ACTIVITY; DNA GYRASE; FLUOROQUINOLONES; QUINOLONES; INHIBITION; DESIGN;

D O I：

10.1016/j.ejmech.2010.11.023

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 8-OCH3 ciprofloxacin methylene and ethylene isatin derivatives with remarkable improvement in lipophilicity were synthesized in this study. These derivatives were evaluated for their in vitro activity against some mycobacteria. All of the synthesized compounds were less active than the parent 8-OCH3 ciprofloxacin against Mycobacteriumsmegmatis CMCC 93202, but most of the methylene isatin derivatives were more active than 8-OCH3 ciprofloxacin, ciprofloxacin, isoniazid and rifampin against MTB H37Rv ATCC 27294. It was noted that compound 3b (MIC: 0.074 mu M) was 2-13 fold more potent than the reference compounds against MTB H37Rv ATCC 27294, and compounds 3f and 3i-k (MIC: 6.72-7.05 mu M) were around 1.6 fold more potent than the parent 8-OCH3 ciprofloxacin, 3.5 fold more potent than ciprofloxacin against MDR-MTB 09710. (C) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：341 / 348

页数：8

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