3-Amino-1-alkyl-cyclopentane carboxamides as small molecule antagonists of the human and murine CC chemokine receptor 2

被引：30

作者：

Butora, Gabor ^{[1
]}

Jiao, Richard ^{[1
]}

Parsons, William H. ^{[1
]}

Vicario, Pasquale P. ^{[1
]}

Jin, Hong ^{[1
]}

Ayala, Julia M. ^{[1
]}

Cascieri, Margaret A. ^{[1
]}

Yang, Lihu ^{[1
]}

机构：

[1] Merck Res Labs, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 13期

关键词：

D O I：

10.1016/j.bmcl.2007.04.053

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of low molecular weight antagonists of both the human and murine CC chemokine receptor 2, containing a l-alkyl-3-(3-methyl-4-spiroindenylpiperidine)-substituted cyclopentanecarboxamide, is described. A SAR study of the C, substituent revealed that short, branched alkyl groups such as isopropyl, isobutyl, or cyclopropyl are optimal for both human and murine CCR2 binding activity. (c) 2007 Elsevier Ltd. All rights reserved.

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页码：3636 / 3641

页数：6

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