Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors

A series of novel tetrahydronaphthyridine-based histamine H3 ligands that have serotonin reuptake transporter inhibitor activity is described. The 1,2,3,4-tetrahydro-2,6-naphthyridine scaffold is assembled via the addition of a nitrostyrene to a metalated pyridine followed by reduction and cyclization to form the naphthyridine. In vitro biological data for these novel compounds are discussed.

Graphical abstractThe synthesis and in vitro activity of novel histamine H3 antagonists with serotonin reuptake activity are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide