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

Bioorganic & Medicinal Chemistry Letters（2012）

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摘要

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.

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关键词

PDE10A,Phosphodiesterase,Hit to lead,Enzyme inhibitor,Naphthyridine

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