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Discovery of N-benzyl-2-[(4S)-4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-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 obesity

✍ Scribed by Richard L. Elliott; Kimberly O. Cameron; Janice E. Chin; Jeremy A. Bartlett; Elena E. Beretta; Yue Chen; Paul Da Silva Jardine; Jeffrey S. Dubins; Melissa L. Gillaspy; Diane M. Hargrove; Amit S. Kalgutkar; Janet A. LaFlamme; Mary E. Lame; Kelly A. Martin; Tristan S. Maurer; Nancy A. Nardone; Robert M. Oliver; Dennis O. Scott; Dexue Sun; Andrew G. Swick; Catherine E. Trebino; Yingxin Zhang

Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 598 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.08.115

No coin nor oath required. For personal study only.

✦ Synopsis

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.

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