Discovery of imidazole carboxamides as potent and selective CCK1R agonists

…, JA Hubert, BV Karanam, SJ Lee, J Pan, S Qian…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 15 p. 4393 - 4396

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Citation Number: 10

Abstract

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.