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

作者	Cameron, KO; Beretta, EE; Chen, Y; Chu-Moyer, M; Fernando, D; Gao, H; Kohrt, J; Lavergne, S; Jardine, PD; Guzman-Perez, A; Hoth, C; Perry, DA; Hadcock, JR; Gautreau, D; Makowski, M; Perez, S; Polivkova, J; Rogers, L; Scott, DO; Swick, AG; Thiede, L; Trebino, CE; Trilles, RV; Wilmowski, J; Zhang, YX

选自	期刊 Bioorganic & Medicinal Chemistry Letters; 卷期 2012年22-8; 页码 2943-2947

关联知识点

[摘要]：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. (C) 2012 Elsevier Ltd. All rights reserved.
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