Design and synthesis of pseudo-symmetric HIV protease inhibitors containing a novel hydroxymethylcarbonyl (HMC)-hydrazide isostere

被引：10

作者：

Hidaka, K

Kimura, T

Hayashi, Y

McDaniel, KF

Dekhtyar, T

Colletti, L

Kiso, Y ^{[1
]}

机构：

[1] Kyoto Pharmaceut Univ, Dept Med Chem, Ctr Frontier Res Med Sci, Yamashima Ku, Kyoto 6078412, Japan

[2] Abbott Labs, Global Pharmaceut Res & Dev, Antiviral Res, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 01期

关键词：

D O I：

10.1016/S0960-894X(02)00848-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Pseudo-symmetric HIV-1 protease inhibitors containing a novel HMC-hydrazide isostere as the transition-state mimic were designed and synthesized. Most of the synthetic compounds with varied structures at the P and P' sites around this core unit showed potent inhibitory activity against HIV-1 protease with nanomolar K-i values. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：93 / 96

页数：4

共 22 条

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