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

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• 作者：Gabor Butora ; Richard Jiao ; William H. Parsons ; Pasquale P. Vicario ; Hong Jin ; Julia M. Ayala ; Margaret A. Cascieri ; Lihu Yang
• 关键词：CCR2 receptor antagonists ; Chemokines
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 出版时间：1 July 2007
• 年：2007
• 卷：17
• 期：13
• 页码：3636-3641
• 全文大小：157 K

文摘

A series of low molecular weight antagonists of both the human and murine CC chemokine receptor 2, containing a 1-alkyl-3-(3-methyl-4-spiroindenylpiperidine)-substituted cyclopentanecarboxamide, is described. A SAR study of the C₁ substituent revealed that short, branched alkyl groups such as isopropyl, isobutyl, or cyclopropyl are optimal for both human and murine CCR2 binding activity.