Pyrrolidine-5,5-trans-lactams.: 4.: Incorporation of a P3/P4 urea leads to potent intracellular inhibitors of hepatitis C virus NS3/4A protease

被引：18

作者：

Slater, MJ ^{[1
]}

Amphlett, EM ^{[1
]}

Andrews, DM ^{[1
]}

Bamborough, P ^{[1
]}

Carey, SJ ^{[1
]}

Johnson, MR ^{[1
]}

Jones, PS ^{[1
]}

Mills, G ^{[1
]}

Parry, NR ^{[1
]}

Somers, DO ^{[1
]}

Stewart, AJ ^{[1
]}

Skarzynski, T ^{[1
]}

机构：

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

来源：

ORGANIC LETTERS | 2003年 / 5卷 / 24期

关键词：

D O I：

10.1021/ol035826v

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

In this, the first of two Letters, we describe how a P3/P4 urea linking unit was used to greatly enhance the biochemical and replicon potency of inhibitors based upon the pyrrolidine-5,5-trans-lactam template. Compound 7b demonstrated a 100 nM IC50 in the replicon cell-based surrogate HCV assay.

引用

页码：4627 / 4630

页数：4

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