Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists

Synthesis, SAR, and binding affinities are described for a new class of 1,8-naphthyridinone CB1 receptor specific inverse agonists. Food intake, knockout mouse, and pharmacokinetic evaluation of 14 indicate that this compound is an effective orally active modulator of CB1.

Graphical abstractThe synthesis, structure–activity relationship, and biological evaluation of a new class of 1,8-naphthyridinone CB1 receptor specific inverse agonists are described.Figure optionsDownload full-size imageDownload as PowerPoint slide