一系列（1H-吡唑-4-基）乙酰胺 P2X7 受体拮抗剂的合成及构效关系研究。
Synthesis and structure-activity relationships of a series of (1H-pyrazol-4-yl)acetamide antagonists of the P2X7 receptor.
机构信息
Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex, CM19 5AW, United Kingdom.
出版信息
Bioorg Med Chem Lett. 2010 May 15;20(10):3161-4. doi: 10.1016/j.bmcl.2010.03.096. Epub 2010 Mar 30.
PMID:20399651
Abstract
High-throughput screening identified compound 1 as a potent P2X(7) receptor antagonist suitable for lead optimisation. Structure-activity relationships (SAR) of a series of (1H-pyrazol-4-yl)acetamides were investigated and compound 32 was identified as a potent P2X(7) antagonist with enhanced potency and favourable physicochemical and pharmacokinetic properties.
摘要
高通量筛选发现化合物 1 是一种有效的 P2X(7)受体拮抗剂，适合进行先导优化。对一系列(1H-吡唑-4-基)乙酰胺的构效关系(SAR)进行了研究，发现化合物 32 是一种有效的 P2X(7)拮抗剂，具有增强的效力和良好的理化和药代动力学性质。
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