Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors

被引：125

作者：

Zhou, Lu

Liu, Ying ^{[1
]}

Zhang, Weilin

Wei, Ping

Huang, Changkang

Pei, Jianfeng

Yuan, Yaxia

Lai, Luhua

机构：

[1] Peking Univ, State Key Lab Struct Chem Unstable & Stable Speci, Coll Chem & Mol Engn, Beijing 100871, Peoples R China

[2] Peking Univ, Ctr Theoret Biol, Beijing 100871, Peoples R China

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2006年 / 49卷 / 12期

关键词：

D O I：

10.1021/jm0602357

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of isatin derivatives were synthesized and tested against SARS CoV 3C-like protease. Substitutions at the N-1 and C-5 positions were examined to elucidate the differences in substrate binding sites of the rhinovirus 3C protease and SARS CoV 3C-like protease. Compound 5f shows significant inhibition with an IC50 of 0.37 mu M. Further study showed that, unlike the irreversible covalent binding of isatin derivatives to human rhinovirus 3C protease, the compounds tested in this study are all noncovalent reversible inhibitors.

引用

页码：3440 / 3443

页数：4

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