Design and synthesis of spiro-cyclopentenyl and spiro-[1,3]-dithiolanyl substituted pyrrolidine-5,5-trans-lactams as inhibitors of hepatitis C virus NS3/4A protease

被引：8

作者：

Andrews, DM ^{[1
]}

Jones, PS ^{[1
]}

Mills, G ^{[1
]}

Hind, SL ^{[1
]}

Slater, MJ ^{[1
]}

Trivedi, N ^{[1
]}

Wareing, KJ ^{[1
]}

机构：

[1] GlaxoSmithKline Med Res Ctr, Stevenage SG1 2NY, Herts, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(03)00274-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Using the pyrrolidine-5,5-trans-lactam template, we have designed small, neutral, mechanism-based inhibitors of hepatitis C NS3/4A protease. Compound 2b, with a spiro-cyclobutyl P1 substituent and an isopropyl carbonyl substituent at the lactam. nitrogen, has an IC50 value in the replicon cell-based assay of 3 muM. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1657 / 1660

页数：4

共 24 条

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