Design, synthesis, and bioevaluation of viral 3C and 3C-like protease inhibitors

被引：47

作者：

Prior, Allan M. ^{[1
]}

Kim, Yunjeong ^{[2
]}

Weerasekara, Sahani ^{[1
]}

Moroze, Meghan ^{[1
]}

Alliston, Kevin R. ^{[3
]}

Uy, Roxanne Adeline Z. ^{[3
]}

Groutas, William C. ^{[3
]}

Chang, Kyeong-Ok ^{[2
]}

Hua, Duy H. ^{[1
]}

机构：

[1] Kansas State Univ, Dept Chem, Manhattan, KS 66506 USA

[2] Kansas State Univ, Coll Vet Med, Dept Diagnost Med & Pathobiol, Manhattan, KS 66506 USA

[3] Wichita State Univ, Dept Chem, Wichita, KS 67260 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 23期

基金：

美国国家科学基金会;

关键词：

Viral 3C and 3C-like protease inhibitors; Norovirus; Human rhinovirus; Severe acute respiratory syndrome; coronavirus; Coronavirus; 229E;

D O I：

10.1016/j.bmcl.2013.09.070

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A class of tripeptidyl transition state inhibitors containing a P1 glutamine surrogate, a P2 leucine, and a P3 arylalanines, was found to potently inhibit Norwalk virus replication in enzyme and cell based assays. An array of warheads, including aldehyde, a-ketoamide, bisulfite adduct, and a-hydroxyphosphonate transition state mimic, was also investigated. Tripeptidyls 2 and 6 possess antiviral activities against noroviruses, human rhinovirus, severe acute respiratory syndrome coronavirus, and coronavirus 229E, suggesting a broad range of antiviral activities. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：6317 / 6320

页数：4

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