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Discovery of imidazole carboxamides as potent and selective CCK1R agonists.

Cheng Zhu, Alexa R Hansen, Thomas Bateman, Zhesheng Chen, Tom G Holt, James A Hubert, Bindhu V Karanam, Susan J Lee, Jie Pan, Su Qian, Vijay B G Reddy, Marc L Reitman, Alison M Strack, Vincent Tong, Drew T Weingarth, Michael S Wolff, Doug J MacNeil, Ann E Weber, Joseph L Duffy, Scott D Edmondson
Bioorganic & Medicinal Chemistry Letters 2008 August 2
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.

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