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

Laura J Chambers, Alexander J Stevens, Andrew P Moses, Anton D Michel, Daryl S Walter, David J Davies, David G Livermore, Elena Fonfria, Emmanuel H Demont, Mythily Vimal, Pam J Theobald, Paul J Beswick, Robert J Gleave, Shilina A Roman, Stefan Senger

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22 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)3161-4
Number of pages4
JournalBioorganic & Medicinal Chemistry Letters
Volume20
Issue number10
DOIs
Publication statusPublished - 15 May 2010

Keywords

  • Acetamides
  • Administration, Oral
  • Animals
  • Anti-Infective Agents
  • High-Throughput Screening Assays
  • Humans
  • Injections, Intravenous
  • Purinergic P2 Receptor Antagonists
  • Pyrazoles
  • Rats
  • Receptors, Purinergic P2
  • Receptors, Purinergic P2X7
  • Structure-Activity Relationship

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