吡啶-3-甲酰胺作为新型用于镇痛的CB(2)激动剂
Pyridine-3-carboxamides as novel CB(2) agonists for analgesia.
作者信息
Mitchell William L, Giblin Gerard M P, Naylor Alan, Eatherton Andrew J, Slingsby Brian P, Rawlings Anthony D, Jandu Karamjit S, Haslam Carl P, Brown Andrew J, Goldsmith Paul, Clayton Nick M, Wilson Alex W, Chessell Iain P, Green Richard H, Whittington Andrew R, Wall Ian D
机构信息
GlaxoSmithKline PLC, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Third Avenue, Harlow, Essex, UK.
出版信息
Bioorg Med Chem Lett. 2009 Jan 1;19(1):259-63. doi: 10.1016/j.bmcl.2008.10.118. Epub 2008 Nov 5.
We describe herein the medicinal chemistry approach which led to the discovery of a novel pyridine-3-carboxamide series of CB(2) receptor agonists. The SAR of this new template was evaluated and culminated in the identification of analogue 14a which demonstrated efficacy in an in vivo model of inflammatory pain.
我们在此描述了导致发现新型吡啶 - 3 - 甲酰胺类CB(2)受体激动剂的药物化学方法。对这个新模板的构效关系进行了评估，最终确定了类似物14a，它在炎症性疼痛的体内模型中显示出疗效。
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