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ID: ALA1157114

Journal: Bioorg Med Chem Lett

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

Authors: Chambers LJ, Stevens AJ, Moses AP, Michel AD, Walter DS, Davies DJ, Livermore DG, Fonfria E, Demont EH, Vimal M, Theobald PJ, Beswick PJ, Gleave RJ, Roman SA, Senger S.

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.

CiteXplore: 20399651

DOI: 10.1016/j.bmcl.2010.03.096