STRUCTURE-BASED DRUG DESIGN OF NONPEPTIDIC P-2 SUBSTITUENTS FOR HIV-1 PROTEASE INHIBITORS

被引：16

作者：

KALISH, VJ ^{[1
]}

TATLOCK, JH ^{[1
]}

DAVIES, JF ^{[1
]}

KALDOR, SW ^{[1
]}

DRESSMAN, BA ^{[1
]}

REICH, S ^{[1
]}

PINO, M ^{[1
]}

NYUGEN, D ^{[1
]}

APPELT, K ^{[1
]}

MUSICK, L ^{[1
]}

WU, BW ^{[1
]}

机构：

[1] ELI LILLY & CO,LILLY RES LABS,INDIANAPOLIS,IN 46285

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 07期

关键词：

D O I：

10.1016/0960-894X(95)00103-Z

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The cocrystal structures of LY289612 and LY297135 were used as a starting point in the design of nonpeptidic HIV-1 protease inhibitors. This report details the discovery of a series of novel aromatic P-2 replacement groups. The 3-hydroxy-2-methyl benzoic acid group, discovered in AG1254, was incorporated into the hydroxyethyl amine series to produce the potent antiviral compound (LY309391/AG1310).

引用

页码：727 / 732

页数：6

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