α-ketoamides, α-ketoesters and α-diketones as HCVNS3 protease inhibitors

被引：75

作者：

Han, W ^{[1
]}

Hu, ZL ^{[1
]}

Jiang, XJ ^{[1
]}

Decicco, CP ^{[1
]}

机构：

[1] Dupont Merck Pharmaceut Co, Expt Stn, Dept Chem & Phys Sci, Wilmington, DE 19880 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(00)00074-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Peptide-based alpha-ketoamides, alpha-ketoesters and alpha-diketones were designed, synthesized and evaluated against HCV NS3 protease. alpha-Ketoamides have the highest affinity among the three classes, with 8 being the most potent inhibitor with an IC50 Of 340 nM. (C) 2000 DuPont Pharmaceuticals Company. Published by Elsevier Science Ltd. All rights reserved.

引用

页码：711 / 713

页数：3

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