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…

文献索引：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

全文：HTML全文

被引用次数: 19

摘要

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.