Design, synthesis, and structure-activity relationship of novel CCR2 antagonists

被引：19

作者：

Kothandaraman, Shankaran ^{[1
]}

Donnely, Karla L. ^{[1
]}

Butora, Gabor ^{[1
]}

Jiao, Richard ^{[1
]}

Pasternak, Alexander ^{[1
]}

Morriello, Gregori J. ^{[1
]}

Goble, Stephen D. ^{[1
]}

Zhou, Changyou ^{[1
]}

Mills, Sander G. ^{[1
]}

MacCoss, Malcolm ^{[1
]}

Vicario, Pasquale P. ^{[2
]}

Ayala, Julia M. ^{[2
]}

DeMartino, Julie A. ^{[2
]}

Struthers, Mary ^{[2
]}

Cascieri, Margaret A. ^{[2
]}

Yang, Lihu ^{[1
]}

机构：

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

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 06期

关键词：

CCR2; Antagonist; Chemotaxis; Aminocyclopentane carboxamide; Reductive aminations; CHEMOATTRACTANT PROTEIN-1 MCP-1; SMALL-MOLECULE; RECEPTOR ANTAGONISTS; CHEMOKINE RECEPTOR-2; HIGHLY POTENT; ATHEROSCLEROSIS; DERIVATIVES; ALCOHOLS; CHEMOTAXIS; DISCOVERY;

D O I：

10.1016/j.bmcl.2008.12.050

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 1-aminocyclopentyl-3-carboxyamides incorporating substituted tetrahydropyran moieties have been synthesized and subsequently evaluated for their antagonistic activity against the human CCR2 receptor. Among them analog 59 was found to posses potent antagonistic activity. (C) 2009 Published by Elsevier Ltd.

引用

页码：1830 / 1834

页数：5

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