Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties

被引：149

作者：

Kim, D

Wang, LP

Hale, JJ

Lynch, CL

Budhu, RJ

MacCross, M

Mills, SG

Malkowitz, L

Gould, SL

DeMartino, JA

Springer, MS

Hazuda, D

Miller, M

Kessler, J

Hrin, RC

Carver, G

Carella, A

Henry, K

Lineberger, J

Schleif, WA

Emini, EA

机构：

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

[2] Merck Res Labs, Dept Immunol Res, Rahway, NJ 07065 USA

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 08期

关键词：

CCR5; HIV-1; antiviral; fused heterocycles;

D O I：

10.1016/j.bmcl.2005.02.030

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists containing a variety of fused heterocycles at the 4-position of the piperidine side chain has been discovered, which are orally bioavailable with potent anti-HIV activity. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：2129 / 2134

页数：6

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