Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-resistant viral strains

被引：24

作者：

Cheng, Y ^{[1
]}

Zhang, FQ

Rano, TA

Lu, ZJ

Schleif, WA

Gabryelski, L

Olsen, DB

Stahlhut, M

Rutkowski, CA

Lin, JH

Jin, LX

Emini, EA

Chapman, KT

Tata, JR

机构：

[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Viral Vaccine Res, West Point, PA 19486 USA

[3] Merck Res Labs, Dept Biol Chem, West Point, PA 19486 USA

[4] Merck Res Labs, Dept Drug Metab, West Point, PA 19486 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 17期

关键词：

D O I：

10.1016/S0960-894X(02)00424-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Indinavir analogues with blocked metabolism sites show highly improved pharmacokinetic profiles in animals. The cis aminochromanol substituted analogues exhibited excellent potency against both the wild-type (NL4-3) virus and protease inhibitor-resistant HIV strains. (C) 2002 Elsevier Science Ltd. All rights reserved.

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页码：2419 / 2422

页数：4

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