Synthesis and evaluation of pyrazolone compounds as SARS-coronavirus 3C-like protease inhibitors

被引：104

作者：

Ramajayam, R. ^{[1
]}

Tan, Kian-Pin ^{[2
]}

Liu, Hun-Ge ^{[2
]}

Liang, Po-Huang ^{[1
,2
]}

机构：

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

[2] Natl Taiwan Univ, Inst Biochem Sci, Taipei 106, Taiwan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 22期

关键词：

Pyrazolone; 3CL protease; SARS-CoV; Coxsackievirus; Computer modeling; RESPIRATORY SYNDROME CORONAVIRUS; 3CL PROTEASE; MAIN PROTEASE; POTENT INHIBITORS; DESIGN; MCI-186; IDENTIFICATION; CINANSERIN; PROTEINASE; ISCHEMIA;

D O I：

10.1016/j.bmc.2010.09.050

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of pyrazolone compounds as possible SARS-CoV 3CL protease inhibitors were designed, synthesized, and evaluated by in vitro protease assay using fluorogenic substrate peptide in which several showed potent inhibition against the 3CL protease. Interestingly, one of the inhibitors was also active against 3C protease from coxsackievirus B3. These inhibitors could be potentially developed into anti-coronaviral and anti-picornaviral agents. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：7849 / 7854

页数：6

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