Novel arylsulfonamides possessing sub-picomolar HIV protease activities and potent anti-HIV activity against wild-type and drug-resistant viral strains

被引：21

作者：

Miller, JF ^{[1
]}

Furfine, ES ^{[1
]}

Hanlon, MH ^{[1
]}

Hazen, RJ ^{[1
]}

Ray, JA ^{[1
]}

Robinson, L ^{[1
]}

Samano, V ^{[1
]}

Spaltenstein, A ^{[1
]}

机构：

[1] GlaxoSmithKline, Res Triangle Pk, NC 27709 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 04期

关键词：

D O I：

10.1016/j.bmcl.2003.12.008

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of P1' chain-extended arylsufonamides was synthesiszed and evaluated for wild-type HIV protease inhibitory activity and in vitro antiviral activity against wild type virus and two protease inhibitor-resistant mutant viruses. All of the compounds showed dramatic increases in enzyme activity as compared to the currently marketed HIV protease inhibitors amprenavir, indinavir, and nelfinavir. In addition, significant improvements in antiviral potencies against wild type and the two mutant viruses were also realized. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：959 / 963

页数：5

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