A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists

Bisaryl cyclic ureas have been identified as high affinity 5-HT2C receptor antagonists with selectivity over 5-HT2A and 5-HT2B. Compounds such as 8 and 22 have shown oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function in rodents.

Graphical abstractA series of novel bisaryl imidazolidinones have been prepared and evaluated both in vitro and in vivo for their 5-HT2C receptor antagonist activity.Figure optionsDownload full-size imageDownload as PowerPoint slide