Synthesis and evaluation of imidazolidinones as nonpeptide HIV-protease inhibitors

被引：15

作者：

DeLucca, GV

机构：

[1] Dupont Merck Pharmaceutical Co., Experimental Station, Wilmington, DE 19880-050 0

来源：

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

关键词：

D O I：

10.1016/S0960-894X(97)00006-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Imidazolidinones were synthesized from 7-membered ring cyclic ureas via a sequential series of novel ring contraction reactions proceeding first through the tetrahydropyrimidinones and finally to the 5-membered ring heterocycle. These imidazolidinones are shown to be excellent HIV-PR inhibitors. The most potent compound 20 having a K-i = 17 nM. (C) 1997 The DuPont Merck Pharmaceutical Company. Published by Elsevier Science Ltd.

引用

页码：495 / 500

页数：6

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