1-Amido-1-phenyl-3-piperidinylbutanes-CCR5 antagonists for the treatment of HIV. Part 1

被引：21

作者：

Barber, Christopher G. ^{[1
]}

Blakemore, David C. ^{[1
]}

Chiva, Jean-Yves ^{[1
]}

Eastwood, Rachel L. ^{[1
]}

Middleton, Donald S. ^{[1
]}

Paradowski, Kerry A. ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Sandwich Labs, Sandwich CT13 9NJ, Kent, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 04期

关键词：

HIV; CCR5; Antiviral; Antagonist; CCR5 RECEPTOR ANTAGONIST; INFECTION; DISCOVERY; MARAVIROC; UK-427,857; AIDS;

D O I：

10.1016/j.bmcl.2009.01.009

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The development of a new class of CCR5 antagonist replacing the tropane core of maraviroc by piperidine with a branched N-substituent is described. Compound 15h shows good whole cell antiviral activity together with microsomal stability and only weak activity at the hERG ion channel. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：1075 / 1079

页数：5

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