合成和评价 3-氨基-6-芳基-哒嗪作为治疗炎性疼痛的选择性 CB(2) 激动剂。
Synthesis and evaluation of 3-amino-6-aryl-pyridazines as selective CB(2) agonists for the treatment of inflammatory pain.
机构信息
Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Cold Harbour Lane, Harlow, Essex CM19 5AW, United Kingdom.
出版信息
Bioorg Med Chem Lett. 2010 Jan 15;20(2):465-8. doi: 10.1016/j.bmcl.2009.11.117. Epub 2009 Nov 27.
A series of 3-amino-6-aryl-pyridazines have been identified as CB(2) agonists with high efficacy and selectivity against the CB(1) receptor. Details of the investigation of structure-activity relationships (SAR) are disclosed, which led to the identification of pyridazine analogue 35, a compound with high potency in an in vivo model of inflammatory pain.
已经确定了一系列 3-氨基-6-芳基-哒嗪类化合物作为 CB(2) 激动剂，它们对 CB(1) 受体具有高效和选择性。本文披露了对构效关系 (SAR) 的研究细节，这导致了哒嗪类似物 35 的鉴定，该化合物在炎症性疼痛的体内模型中具有高效力。
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