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Discovery of imidazole carboxamides as potent and selective CCK1R agonists |
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| Authors: | 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 |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA. cheng_zhu@merck.com |
| 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. |
| Keywords: | CCK1R agonist Obesity Cholecystokinin Food intake reduction 1 2-Diaryl imidazole |
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