DESIGN, SYNTHESIS, AND ACTIVITY OF CONFORMATIONALLY-CONSTRAINED MACROCYCLIC PEPTIDE-BASED INHIBITORS OF HIV PROTEASE

被引：18

作者：

SMITH, RA ^{[1
]}

COLES, PJ ^{[1
]}

CHEN, JJ ^{[1
]}

ROBINSON, VJ ^{[1
]}

MACDONALD, ID ^{[1
]}

CARRIERE, J ^{[1
]}

KRANTZ, A ^{[1
]}

机构：

[1] SYNTEX RES CANADA,MISSISSAUGA,ON,CANADA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(00)80074-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Conformationally-constrained macrocyclic peptide-based hydroxyethylamines, with 17- to 19-membered ring systems, have been designed and synthesized as HIV protease inhibitors. Structure-activity relationships were consistent with molecular modeling studies, and certain cyclic inhibitors were developed with HIV protease IC50 values of similar to-1 nM, and antiviral activities (HIV-1/RF infected MT-2 cells) of EC(50) 4-8 nM.

引用

页码：2217 / 2222

页数：6

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