Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors

被引：178

作者：

Chen, LR

Wang, YC

Lin, YW

Chou, SY

Chen, SF

Liu, LT

Wu, YT

Chih-Jung, KB

Chen, TSS

Juang, SH

机构：

[1] Dev Ctr Biotechnol, Taipei, Taiwan

[2] Acad Sinica, Inst Biol Chem, Taipei 11529, Taiwan

[3] Acad Sinica, Genom Res Ctr, Taipei 11529, Taiwan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 12期

关键词：

SARS CoV protease inhibitor; isatin;

D O I：

10.1016/j.bmcl.2005.04.027

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

N-Substituted isatin derivatives were prepared from the reaction of isatin and various bromides via two steps. Bioactivity assay results (in vitro tests) demonstrated that some of these compounds are potent and selective inhibitors against SARS coronavirus 3CL protease with IC50 values ranging from 0.95 to 17.50 mu M. Additionally, isatin 4o exhibited more potent inhibition for SARS coronavirus protease than for other proteases including papain, chymotrypsin, and trypsin. (c) 2005 Elsevier Ltd. All rights reserved.

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收藏

页码：3058 / 3062

页数：5

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