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

Udo Bauer; Fabrizio Giordanetto; Martin Bauer; Gavin O'Mahony; Kjell E Johansson; Wolfgang Knecht; Judith Hartleib-Geschwindner; Eva Töppner Carlsson; Cristofer Enroth

doi:10.1016/j.bmcl.2012.01.046

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

Research output: Contribution to journal › Article

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 language	English
Pages (from-to)	1944-1948
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	22
Issue number	5
Publication status	Published - 2012 Mar 1
Publication category	Research
Peer-reviewed	Yes
Externally published	Yes

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

Abstract

Details

Keywords

DOI