Pharmacological Evaluation of Novel Bioisosteres of an Adamantanyl Benzamide P2X7 Receptor Antagonist

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Wilkinson, Shane M; Barron, Melissa L; O'Brien-Brown, James; Janssen, Bieneke; Stokes, Leanne; Werry, Eryn L; Chishty, Mansoor; Skarratt, Kristen K; Ong, Jennifer A; Hibbs, David E; Vugts, Danielle J; Fuller, Stephen; Windhorst, Albert D; Kassiou, Michael;
  • Related identifiers: doi: 10.1021/acschemneuro.7b00272
  • Subject: P2X7 | single nucleotide polymorphisms (SNPs) | metabolism | pharmacokinetic | central nervous system (CNS) | bioisostere

Abstract Adamantanyl benzamide 1 was identified as a potent P2X7R antagonist but failed to progress further due to poor metabolic stability. We describe the synthesis and SAR of a series of bioisosteres of benzamide 1 to explore improvements in the pharmacological p... View more
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