Design and synthesis of cinanserin analogs as severe acute respiratory syndrome coronavirus 3CL protease inhibitors

被引：23

作者：

Yang, Qiangang ^{[1
]}

Chen, Lill ^{[1
]}

He, Xuchang ^{[1
]}

Gao, Zhenting ^{[2
]}

Bai, Donglu ^{[1
]}

机构：

[1] Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China

[2] E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2008年 / 56卷 / 10期

关键词：

SARS coronavirus 3CL protease; cinanserin analogs; inhibitor; fluorescence resonance energy transfer-based assay;

D O I：

10.1248/cpb.56.1400

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The severe acute respiratory syndrome (SARS) coronavirus 3CL protease is an attractive target for the development of anti-SARS drugs. In this paper, cinanserin (1) analogs were synthesized and tested for the in-hibitory activities against SARS-coronavirus (CoV) 3CL protease by fluorescence resonance energy transfer (FRET) assay. Four analogs show significant activities, especially compound 26 with an IC50 of 1.06 mu M.

引用

页码：1400 / 1405

页数：6

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