Synthesis and structure–activity relationships of a series of (1H-pyrazol-4-yl) acetamide antagonists of the P2X 7 receptor

LJ Chambers, AJ Stevens, AP Moses, AD Michel…

Index: Chambers, Laura J.; Stevens, Alexander J.; Moses, Andrew P.; Michel, Anton D.; Walter, Daryl S.; Davies, David J.; Livermore, David G.; Fonfria, Elena; Demont, Emmanuel H.; Vimal, Mythily; Theobald, Pam J.; Beswick, Paul J.; Gleave, Robert J.; Roman, Shilina A.; Senger, Stefan Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 10 p. 3161 - 3164

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Citation Number: 19

Abstract

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.