Potent inhibitors of the hepatitis C virus NS3 protease:: Use of a novel P2 cyclopentane-derived template

被引：19

作者：

Johansson, Per-Ola

Back, Marcus

Kvarnstrom, Ingemar

Jansson, Katarina

Vrang, Lotta

Hamelink, Elizabeth

Hallberg, Anders

Rosenquist, Asa ^{[1
]}

Samuelsson, Bertil

机构：

[1] Linkoping Univ, Dept Chem, S-58183 Linkoping, Sweden

[2] Medivir AB, S-14144 Huddinge, Sweden

[3] Uppsala Univ, BMC, Dept Med Chem, S-75123 Uppsala, Sweden

[4] Stockholm Univ, Arrhenius Lab, Dept Organ Chem, S-10691 Stockholm, Sweden

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 15期

关键词：

HCV; NS3; protease inhibitor; cyclopentane-derived P2 scaffold;

D O I：

10.1016/j.bmc.2006.04.008

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：

The HCV NS3 protease is essential for replication of the hepatitis C virus (HCV) and therefore constitutes a promising new drug target for anti-HCV therapy. Several potent and promising HCV NS3 protease inhibitors, some of which display low nanomolar activities, were identified from a series of novel inhibitors incorporating a trisubstituted cyclopentane dicarboxylic acid moiety as a surrogate for the widely used N-acyl-(4R)-hydroxyproline in the P2 position. (c) 2006 Elsevier Ltd. All rights reserved.

引用

收藏

页码：5136 / 5151

页数：16

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