Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. Part 7: Structure-activity studies of bicyclic 2-pyridone-containing peptidomimetics

被引：68

作者：

Dragovich, PS ^{[1
]}

Prins, TJ ^{[1
]}

Zhou, R ^{[1
]}

Johnson, TO ^{[1
]}

Brown, EL ^{[1
]}

Maldonado, FC ^{[1
]}

Fuhrman, SA ^{[1
]}

Zalman, LS ^{[1
]}

Patick, AK ^{[1
]}

Matthews, DA ^{[1
]}

Hou, XJ ^{[1
]}

Meador, JW ^{[1
]}

Ferre, RA ^{[1
]}

Worland, ST ^{[1
]}

机构：

[1] Agouron Pharmaceut Inc, Pfizer Global Res & Dev La Jolla, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(02)00008-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The structure-based design, chemical synthesis. and biological evaluation of bicyclic 2-pyridone-containing human rhinovirus (HRV) 3C protease (3CP) inhibitors are described. An optimized compound is shown to exhibit antiviral activity when tested against a variety of HRV serotypes (EC50's ranging from 0.037 to 0.162 muM). (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：733 / 738

页数：6