Discovery of 4-hydroxy-1,6-naphthyridine-3-carbonitrile derivatives as novel PDE10A inhibitors

Research output: Contribution to journalArticle

Abstract

A series of 1,6-naphthyridine-based compounds was synthesized as potent phosphodiesterase 10A (PDE10A) inhibitors. Structure-based chemical modifications of the discovered chemotype served to further improve potency and selectivity over DHODH, laying the foundation for future optimization efforts.

Details

Authors
  • Udo Bauer
  • Fabrizio Giordanetto
  • Martin Bauer
  • Gavin O'Mahony
  • Kjell E Johansson
  • Wolfgang Knecht
  • Judith Hartleib-Geschwindner
  • Eva Töppner Carlsson
  • Cristofer Enroth
External organisations
  • AstraZeneca, Sweden
Research areas and keywords

Keywords

  • Antipsychotic Agents/chemistry, Humans, Models, Molecular, Naphthyridines/chemistry, Nitriles/chemistry, Phosphodiesterase Inhibitors/chemistry, Phosphoric Diester Hydrolases/chemistry, Structure-Activity Relationship
Original languageEnglish
Pages (from-to)1944-1948
JournalBioorganic & Medicinal Chemistry Letters
Volume22
Issue number5
Publication statusPublished - 2012 Mar 1
Publication categoryResearch
Peer-reviewedYes
Externally publishedYes