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
收藏
页码：1400 / 1405
页数：6
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