Synthesis of 3-phenylsulfonylmethyl cyclohexylaminobenzamide-derived antagonists of CC chemokine receptor 2 (CCR2)

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• 作者：Michael G. Yang ; Zili Xiao ; Qing Shi ; Robert J. Cherney ; Andrew J. Tebben ; George V. De Lucca ; Joseph B. Santella III ; Ruowei Mo ; Mary Ellen Cvijic ; Qihong Zhao ; Joel C. Barrish ; Percy H. Carter ; ^{percy.carter@bms.com}
• 关键词：CCR2 ; Chemokine ; GPCR ; Antagonist
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 出版时间：1 February, 2012
• 年：2012
• 卷：22
• 期：3
• 页码：1384-1387
• 全文大小：419 K

文摘

We report the synthesis of 3-phenylsulfonylmethyl cyclohexylaminobenzamides (class=""boldFont"">4) as CCR2 inhibitors for the potential treatment of inflammatory diseases. Several of the compounds display nanomolar binding affinity for CCR2. The in vitro structure-activity relationships of class=""boldFont"">4 are described, and are also reconciled with those from the related 2-phenylsulfonylmethyl series.