3-[2-(N-苯乙酰胺)]-1,5-苯并二氮杂卓类：口服活性、具有结合选择性的胆囊收缩素-A激动剂。
3-[2-(N-phenylacetamide)]-1,5-benzodiazepines: orally active, binding selective CCK-A agonists.
作者信息
Willson T M, Henke B R, Momtahen T M, Myers P L, Sugg E E, Unwalla R J, Croom D K, Dougherty R W, Grizzle M K, Johnson M F, Queen K L, Rimele T J, Yingling J D, James M K
机构信息
Glaxo Wellcome Research and Development, Research Triangle Park, North Carolina 27709, USA.
出版信息
J Med Chem. 1996 Jul 19;39(15):3030-4. doi: 10.1021/jm960205b.
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.
对1,5-苯二氮䓬CCK - A激动剂1的C - 3取代基进行了一系列修饰。将内部脲NH替换并添加一个甲基以生成C - 3季碳，得到乙酰胺6，其在体外表现出CCK - A受体结合选择性和亚微摩尔激动剂活性。苯二氮䓬6在体内小鼠胆囊排空试验中具有活性，是一种新型的口服活性、结合选择性CCK - A激动剂。
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