P1 phenethyl peptide boronic acid inhibitors of HCVNS3 protease

被引：55

作者：

Priestley, ES ^{[1
]}

De Lucca, I ^{[1
]}

Ghavimi, B ^{[1
]}

Erickson-Viitanen, S ^{[1
]}

Decicco, CP ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Expt Stn, Wilmington, DE 19880 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 21期

关键词：

D O I：

10.1016/S0960-894X(02)00682-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of peptide boronic acids containing extended, hydrophobic P1 residues was prepared to probe the shallow, hydrophobic S1 region of HCV NS3 protease. The p-trifluoromethylphenethyl P1 substituent was identified as optimal with respect to inhibitor potency for NS3 and selectivity against elastase and chymotrypsin. (C) 2002 Published by Elsevier Science Ltd.

引用

页码：3199 / 3202

页数：4

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