STUDIES ON ORALLY AVAILABLE INHIBITORS OF HIV PROTEASE - PEPTIDYL ALDEHYDES AND TRIFLUOROMETHYL KETONES

被引：10

作者：

HODGE, CN

ALDRICH, PE

FERNANDEZ, CH

OTTO, MJ

RAYNER, MM

WONG, YN

ERICKSONVIITANEN, S

机构：

[1] DUPONT MERCK PHARMACEUT CO,DEPT VIROL RES,WILMINGTON,DE 19880

[2] DUPONT MERCK PHARMACEUT CO,DEPT DRUG METAB,WILMINGTON,DE 19880

来源：

ANTIVIRAL CHEMISTRY & CHEMOTHERAPY | 1994年 / 5卷 / 04期

关键词：

D O I：

10.1177/095632029400500407

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Low-molecular-weight peptidyl aldehyde inhibitors of HIV protease that reach in vivo plasma concentrations after oral administration substantially in excess of the antiviral IC90 are described. We also report efforts to improve the potency and stability of these compounds that culminated in a series of peptidyl trifluoromethyl ketones with increased potency but decreased bioavailability.

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收藏

页码：257 / 262

页数：6

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