Simple cis-epoxide-based inhibitors of HIV-1 protease

被引：12

作者：

Abell, AD ^{[1
]}

Hoult, DA ^{[1
]}

Bergman, DA ^{[1
]}

Fairlie, DP ^{[1
]}

机构：

[1] UNIV QUEENSLAND,CTR DRUG DESIGN & DEV,BRISBANE,QLD 4072,AUSTRALIA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 22期

关键词：

D O I：

10.1016/S0960-894X(97)10106-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The 4-nitrophenoxy-based epoxide 6a, conveniently synthesized using Sharpless epoxidation chemistry, has been shown to be an irreversible inhibitor of HIV-1, protease (K-inact 1.8 mu M, pH 6.5, I = 0.1 M). Related analogues, differing in the mode of attachment to the epoxide core, have also been prepared and assayed against HIV-1 protease. (C) 1997 Elsevier Science Ltd.

引用

页码：2853 / 2856

页数：4

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