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Synthesis and structure-activity relationships of a series of (1H-pyrazol-4-yl)acetamide antagonists of the P2X7 receptor.
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.
Affiliation
  • Chambers LJ; Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex, CM19 5AW, United Kingdom. laura.j.chambers@gsk.com
Bioorg Med Chem Lett ; 20(10): 3161-4, 2010 May 15.
Article in En | MEDLINE | ID: mdl-20399651
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.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrazoles / Purinergic P2 Receptor Antagonists / Acetamides / Anti-Infective Agents Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2010 Document type: Article Affiliation country: United kingdom
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrazoles / Purinergic P2 Receptor Antagonists / Acetamides / Anti-Infective Agents Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2010 Document type: Article Affiliation country: United kingdom