Discovery of novel phosphonate derivatives as hepatitis C virus NS3 protease inhibitors

被引：43

作者：

Sheng, X. Christopher ^{[1
]}

Pyun, Hyung-Jung ^{[1
]}

Chaudhary, Kleem ^{[1
]}

Wang, Jianying ^{[1
]}

Doerffler, Edward ^{[1
]}

Fleury, Melissa ^{[1
]}

McMurtrie, Darren ^{[1
]}

Chen, Xiaowu ^{[1
]}

Delaney, William E. ^{[1
]}

Kim, Choung U. ^{[1
]}

机构：

[1] Gilead Sci Inc, Foster City, CA 94404 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 13期

关键词：

HCV NS3 protease inhibitors; Phosphonate as caboxylate replacement; ANALOGS;

D O I：

10.1016/j.bmcl.2009.05.023

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel class of phosphonate derivatives was designed to mimic the interaction of product-like carboxylate based inhibitors of HCV NS3 protease. A phosphonic acid (compound 2) was demonstrated to be a potent HCV NS3 protease inhibitor, and a potential candidate for treating HCV infection. The syntheses and preliminary biological evaluation of this phosphonate class of inhibitor are described. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：3453 / 3457

页数：5

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