Naphthyl piperazines with dual activity as 5-HT1D antagonists and 5-HT reuptake inhibitors

SAR around a known molecule with dual 5-HT1D antagonist and 5-HTtransporter inhibitory activity has led to the discovery of molecules with improved dual activity and reduced cross-reactivity toward other aminergic receptors (5-HT1B, α1, and D2).

Graphical abstractA series of compounds with dual activity as 5-HT1D antagonists and 5-HT reuptake inhibitors were prepared by incorporating naphthylpiperazines to substituted isochromans and dihydroisobenzofurans.Figure optionsDownload full-size imageDownload as PowerPoint slide