Synthesis and structure–activity relationships of a series of (1H-pyrazol-4-yl)acetamide antagonists of the P2X₇ receptor

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• 作者：Laura J. Chambers ; Alex ; er J. Stevens ; Andrew P. Moses ; Anton D. Michel ; Daryl S. Walter ; David J. Davies ; David G. Livermore ; Elena Fonfria ; Emmanuel H. Demont ; Mythily Vimal ; Pam J. Theobald ; Paul J
• 关键词：P2X7 ; P2X7 antagonist ; Lead optimisation
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：15 May 2010
• 年：2010
• 卷：20
• 期：10
• 页码：3161-3164
• 全文大小：2000 K

文摘

High-throughput screening identified compound 1 as a potent P2X₇ 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 P2X₇ antagonist with enhanced potency and favourable physicochemical and pharmacokinetic properties.