ISOPHTHALIC ACID-DERIVATIVES - AMINO-ACID SURROGATES FOR THE INHIBITION OF HIV-1 PROTEASE

被引：17

作者：

KALDOR, SW ^{[1
]}

DRESSMAN, BA ^{[1
]}

HAMMOND, M ^{[1
]}

APPELT, K ^{[1
]}

BURGESS, JA ^{[1
]}

LUBBEHUSEN, PP ^{[1
]}

MUESING, MA ^{[1
]}

HATCH, SD ^{[1
]}

WISKERCHEN, MA ^{[1
]}

BAXTER, AJ ^{[1
]}

机构：

[1] AGOURON PHARMACEUT INC,SAN DIEGO,CA 92121

来源：

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

关键词：

D O I：

10.1016/0960-894X(95)00102-Y

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Using the X-ray crystal structure of the inhibitor 1 complexed to HIV-1 protease, a new series of HIV-1 protease inhibitors was developed incorporating substituted isophthalic acid derivatives as amino acid surrogates. Through iterative structure-based design, the lead compound 2 was optimized to produce a variety of non-peptide HIV-1 protease inhibitors with significant antiviral activity. In contrast to 1, several members of this series exhibit significant oral absorption in animals.

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收藏

页码：721 / 726

页数：6

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