New spiro-piperidines as 5-HT2B receptor antagonists

A functional screening highlighted a series of spiro-piperidines as 5-HT2B receptor antagonists. Preliminary structure–activity relationship has been explored driving to potent antagonists (IC50 = 1 nM) and indicating directions for further explorations.

The synthesis of the compound 45 (IC50 = 1.8 nM) and its analogs is reported.Figure optionsDownload as PowerPoint slide