期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 24, 页码 7278-7282出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.10.080
关键词
Antitubercular activity; Mycobacterium tuberculosis; Azomethine ylide; 1,3-Dipolar cycloaddition; 2-Arylidene-1,3-indanediones; Dispiro-oxindolylpyrrolothiazoles
资金
- Department of Science and Technology, New Delhi [DST/INT/SPAIN/09]
- University Grants Commission, New Delhi [36-155/2008(SR)]
A facile 1,3-dipolar cycloaddition of azomethine ylide generated in situ from the reaction of 1,3-thiazolane-4-carboxylic acid and isatin to 2-arylidene-1,3-indanediones furnished novel dispiro-oxindolylpyrrolothiazoles regio- and stereo-selectively in moderate to good yields (60-92%). In vitro antitubercular screening of 27 compounds against Mycobacterium tuberculosis H37Rv (MTB) disclosed that spiro[5.3']-5'-nitrooxindolespiro-[6.3 '']-1H-inden-1 '',3 ''(2H)-dione-7-(4-bromophenyl)tetrahydro-1H-pyrrolo[1,2-c] [1,3] thiazole has the maximum potency with a minimum inhibitory concentration (MIC) of 1.4 mu M against MTB, being 3.4 and 5.4 times more potent than ciprofloxacin and ethambutol, respectively. (C) 2010 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据