Structure-based design of ketone-containing, tripeptidyl human rhinovirus 3C protease inhibitors

被引：40

作者：

Dragovich, PS

Zhou, R

Webber, SE

Prins, TJ

Kwok, AK

Okano, K

Fuhrman, SA

Zalman, LS

Maldonado, FC

Brown, EL

Meador, JW

Patick, AK

Ford, CE

Brothers, MA

Binford, SL

Matthews, DA

Ferre, RA

Worland, ST

机构：

[1] Agouron Pharmaceut Inc, San Diego, CA 92121 USA

[2] Japan Tobacco Inc, Cent Pharmaceut Res Inst, Osaka 56911, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 01期

关键词：

D O I：

10.1016/S0960-894X(99)00587-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Tripeptide-derived molecules incorporating C-terminal ketone electrophiles were evaluated as reversible inhibitors of the cysteine-containing human rhinovirus 3C protease (3CP). An optimized example of such compounds displayed potent 3CP inhibition activity (K-i = 0.0045 mu M) and in vitro antiviral properties (EC50 = 0.34 mu M) when tested against HRV serotype-14. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：45 / 48

页数：4

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