Substituted dipiperidine alcohols as potent CCR2 antagonists

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• 作者：Mingde Xia ; Cuifen Hou ; Duane DeMong ; Scott Pollack ; Meng Pan ; James Brackley ; Monica Singer ; Michele Matheis ; Druie Cavender ; Michael Wachter
• 关键词：Chemokines ; MCP-1 ; CCR2 antagonist
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2008
• 出版时间：15 June 2008
• 年：2008
• 卷：18
• 期：12
• 页码：3562-3564
• 全文大小：153 K

文摘

The synthesis and biological evaluation of a series of substituted dipiperidine alcohols are described. Structure–activity relationship studies led to the discovery of potent CCR2 antagonists displaying IC₅₀ values in the nanomolar or subnanomolar range. The cinnamoyl compounds had higher binding affinities than the corresponding urea analogs.