Discovery of imidazole carboxamides as potent and selective CCK1R agonists

High-throughput screening revealed diaryl pyrazole 3 as a selective albeit modest cholecystokinin 1 receptor (CCK1R) agonist. SAR studies led to the discovery and optimization of a novel class of 1,2-diaryl imidazole carboxamides. Compound 44, which was profiled extensively, showed good in vivo mouse gallbladder emptying (mGBE) and lean mouse overnight food intake (ONFI) reduction activities.

The discovery and optimization of a novel class of 1,2-diaryl imidazole carboxamides as CCK1R agonists are reported. Compound 44 exhibited excellent lean mouse overnight food intake reduction.Figure optionsDownload as PowerPoint slide