1.
J Med Chem
; 39(15): 3030-4, 1996 Jul 19.
Article
in English
| MEDLINE
| ID: mdl-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.
Subject(s)
Acetanilides , Azepines/chemical synthesis , Cholecystokinin/agonists , Animals , Azepines/metabolism , Azepines/pharmacology , Gallbladder/drug effects , Gallbladder/physiology , Guinea Pigs , Mice , Molecular Structure , Muscle Contraction/drug effects , Receptors, Cholecystokinin/metabolism
2.
J Med Chem
; 37(11): 1550-2, 1994 May 27.
Article
in English
| MEDLINE
| ID: mdl-8201587
