… -dihydro-6H-[1, 2, 4] triazolo [4, 3-a][1, 5] benzodiazepin-6-yl]-N-isopropylacetamide, an orally active, gut-selective CCK1 receptor agonist for the potential treatment of …

…, KO Cameron, JE Chin, JA Bartlett, EE Beretta…

文献索引：Elliott, Richard L.; Cameron, Kimberly O.; Chin, Janice E.; Bartlett, Jeremy A.; Beretta, Elena E.; Chen, Yue; Jardine, Paul Da Silva; Dubins, Jeffrey S.; Gillaspy, Melissa L.; Hargrove, Diane M.; Kalgutkar, Amit S.; Laflamme, Janet A.; Lame, Mary E.; Martin, Kelly A.; Maurer, Tristan S.; Nardone, Nancy A.; Oliver, Robert M.; Scott, Dennis O.; Sun, Dexue; Swick, Andrew G.; Trebino, Catherine E.; Zhang, Yingxin Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 22 p. 6797 - 6801

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被引用次数: 13

摘要

We describe the design, synthesis, and structure–activity relationships of triazolobenzodiazepinone CCK1 receptor agonists. Analogs in this series demonstrate potent agonist activity as measured by in vitro and in vivo assays for CCK1 agonism. Our efforts resulted in the identification of compound 4a which significantly reduced food intake with minimal systemic exposure in rodents.