Discovery of imidazole carboxamides as potent and selective CCK1R agonists

作者：Zhu Cheng^*; Hansen Alexa R; Bateman Thomas; Chen Zhesheng; Holt Tom G; Hubert James A; Karanam Bindhu V; Lee Susan J; Pan Jie; Qian Su; Reddy Vijay B G; Reitman Marc L; Strack Alison M; Tong Vincent; Weingarth Drew T; Wolff Michael S; MacNeil Doug J; Weber Ann E; Duffy Joseph L; Edmondson Scott D

来源：Bioorganic & Medicinal Chemistry Letters, 2008, 18(15): 4393-4396.

DOI：10.1016/j.bmcl.2008.06.057

• CCK1R agonist
• obesity
• cholecystokinin
• food intake reduction
• 1,2-diaryl imidazole

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 pro. led extensively, showed good in vivo mouse gallbladder emptying (mGBE) and lean mouse overnight food intake (ONFI) reduction activities.

• 出版日期2008-8-1