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  • Title: 3-[2-(N-phenylacetamide)]-1,5-benzodiazepines: orally active, binding selective CCK-A agonists.
    Author: Willson TM, Henke BR, Momtahen TM, Myers PL, Sugg EE, Unwalla RJ, Croom DK, Dougherty RW, Grizzle MK, Johnson MF, Queen KL, Rimele TJ, Yingling JD, James MK.
    Journal: J Med Chem; 1996 Jul 19; 39(15):3030-4. PubMed ID: 8709137.
    Abstract:
    A series of modifications were made to the C-3 substituent of the 1,5-benzodiazepine CCK-A agonist 1. Replacement of the inner urea NH and addition of a methyl group to generate a C-3 quaternary carbon resulted in acetamide 6, which showed CCK-A receptor binding selectivity and sub-micromolar agonist activity in vitro. Benzodiazepine 6 was active in an in vivo mouse gallbladder emptying assay and represents a novel orally active, binding selective CCK-A agonist.
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