… -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…

Index: 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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Citation Number: 13

Abstract

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.