Lead identification of 2-iminobenzimidazole antagonists of the chemokine receptor CXCR3

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• 作者：Martin E. Hayes ; Eric C. Breinlinger ; Grier A. Wallace ; Pintipa Grongsaard ; Wenyan Miao ; Michael J. McPherson ; Robert H. Stoffel ; David W. Green ; Gregory P. Roth
• 关键词：Chemokine ; Chemokine antagonist ; CXCR3 ; IP-10 ; CXCL10 ; Multiple sclerosis ; Benzimidazole ; 2-Iminobenzimidazole
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2008
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 April 2008
• 卷：18
• 期：7
• 页码：2414-2419
• 文件大小：220 K

摘要

Modification of a 2-iminobenzimidazole series derived from an HTS hit resulted in compounds with improved in-vitro species selectivity. Incorporation of an 8-quinoline amide and conformational rigidification of an aliphatic tether furnished potent compounds suitable for further lead optimization.