SYNTHESIS AND ANTIVIRAL ACTIVITY OF A NOVEL CLASS OF HIV-1 PROTEASE INHIBITORS CONTAINING A HETEROCYCLIC P-1'-P-2' AMIDE BOND ISOSTERE

被引：48

作者：

THOMPSON, SK ^{[1
]}

EPPLEY, AM ^{[1
]}

FRAZEE, JS ^{[1
]}

DARCY, MG ^{[1
]}

LUM, RT ^{[1
]}

TOMASZEK, TA ^{[1
]}

IVANOFF, LA ^{[1
]}

MORRIS, JF ^{[1
]}

STERNBERG, EJ ^{[1
]}

LAMBERT, DM ^{[1
]}

FERNANDEZ, AV ^{[1
]}

PETTEWAY, SR ^{[1
]}

MEEK, TD ^{[1
]}

METCALF, BW ^{[1
]}

GLEASON, JG ^{[1
]}

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT INC,DEPT MOLEC VIROL & HOST DEF,KING OF PRUSSIA,PA 19406

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(01)80406-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of hydroxyethylene-based peptidomimetics that contain 2-substituted nitrogen heterocycles as P-1'-P-2' amide bond isosteres has been prepared and evaluated as inhibitors of HIV-1 protease and in vitro HIV-1 replication. Many of these compounds exhibit inhibition constants in the low to subnanomolar range. Structure-activity relationships are discussed.

引用

页码：2441 / 2446

页数：6

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