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Doc ID CHEMBL1157114
Journal Bioorg. Med. Chem. Lett. (2010) 20:3161-3164
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
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