Tetrahydroisoquinolines as MCH-R1 antagonists

A series of potent and selective inhibitors of h-MCH-R1 has been developed based on the piperidine glycineamide compounds I and II. These structurally more rigid tetrahydroisoquinolines (III and IV) showed better pharmacokinetics. The highly potent compounds 12d and 12g displayed excellent rat pk.

A series of potent and selective MCH-R1 antagonists have been discovered based on a piperidine glycineamide series.Figure optionsDownload as PowerPoint slide