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

Bioorganic & Medicinal Chemistry Letters(2011)

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摘要
We report the design, synthesis, and SAR of triazolobenzodiazepinone CCK1 receptor agonists. Compound 4a is a potent, selective CCK1 receptor agonist which reduces food intake in rodents with minimal systemic exposure.
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关键词
CCK,Cholecystokinin,CCK1R,Gut selective,Triazolobenzodiazepinone
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