Synthesis and evaluation of delta lactams as nonpeptide HIV-protease inhibitors

被引：22

作者：

DeLucca, GV

机构：

[1] Dupont Merck Pharmaceutical Company, Experimental Station, Wilmington, DE 19880-0500

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(97)00007-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The cyclization of the linear hydroxyethylene isostere based HIV-PR inhibitors gave the delta lactam XQ921, which was found to have a K-i = 9.4 uM. It is proposed that a major reason for the weaker potency of the lactam XQ921 compared to cyclic urea based inhibitors is the lack of a P1' substituent that could interact with the S1' pocket of HIV-PR. (C) 1997 The DuPont Merck Pharmaceutical Company. Published by Elsevier Science Ltd.

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页码：501 / 504

页数：4

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