Studies on the C-terminal of hexapeptide inhibitors of the hepatitis C virus serine protease

被引：90

作者：

Llinàs-Brunet, M ^{[1
]}

Bailey, M ^{[1
]}

Déziel, R ^{[1
]}

Fazal, G ^{[1
]}

Gorys, V ^{[1
]}

Goulet, S ^{[1
]}

Halmos, T ^{[1
]}

Maurice, R ^{[1
]}

Poirier, M ^{[1
]}

Poupart, MA ^{[1
]}

Rancourt, J ^{[1
]}

Thibeault, D ^{[1
]}

Wernic, D ^{[1
]}

Lamarre, D ^{[1
]}

机构：

[1] Boehringer Ingelheim Ltd, Biomega Res Div, Laval, PQ H7S 2G5, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 19期

关键词：

D O I：

10.1016/S0960-894X(98)00480-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Replacememt of the C-terminal carboxylic acid functionality of peptide inhibitors of hepatitis C virus (HCV) NS3 protease (complexed with NS4A peptide cofactor) by activated carbonyl groups does not produce any substantial increase in potency. These latter inhibitors also inhibit a variety of other serine and cysteine proteases whereas the carboxylic acids are specific. Norvaline was identified as a chemically stable replacement for the P1 residue of Ac-DDIVPC-OH which was also compatible with activated carbonyl functionalities. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：2719 / 2724

页数：6

共 31 条

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