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. 2012 Apr 15;22(8):2943-7.
doi: 10.1016/j.bmcl.2012.02.049. Epub 2012 Feb 23.

Discovery of new piperidine amide triazolobenzodiazepinones as intestinal-selective CCK1 receptor agonists

Kimberly O Cameron  1 , Elena E Beretta, Yue Chen, Margaret Chu-Moyer, Dilinie Fernando, Hua Gao, Jeffrey Kohrt, Sophie Lavergne, Paul Da Silva Jardine, Angel Guzman-Perez, Christopher Hoth, David A Perry, John R Hadcock, Denise Gautreau, Michael Makowski, Sylvie Perez, Jana Polivkova, Lucy Rogers, Dennis O Scott, Andrew G Swick, Lucinda Thiede, Catherine E Trebino, Richard V Trilles, Julie Wilmowski, Yingxin Zhang
Affiliations

Discovery of new piperidine amide triazolobenzodiazepinones as intestinal-selective CCK1 receptor agonists

Kimberly O Cameron et al. Bioorg Med Chem Lett. .

Abstract

New cholecystokinin-1 receptor (CCK1R) agonist 'triggers' were identified using iterative library synthesis. Structural activity relationship studies led to the discovery of compound 10e, a potent CCK1R agonist that demonstrated robust weight loss in a diet-induced obese rat model with very low systemic exposure. Pharmacokinetic data suggest that efficacy is primarily driven through activation of CCK1R's located within the intestinal wall.

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