Novel design of nonpeptide AVP V-2 receptor agonists: Structural requirements for an agonist having 1-(4-aminobenzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepine as a template

The discovery of a series of nonpeptide arginine vasopressin V-2 receptor a gonists is described. After identifying the aniline derivative 8 as our lea d compound from the metabolites of compound 7 that showed antidiuretic acti vity by po administration to Brattleboro rats, improvements in the in vitro potency involving evaluations of the structural requirements for agonist a ction and optimizing the structure of the benzoyl moiety have been intensiv ely undertaken. These studies led to compounds leg, 19a, and 23b,h,i that s how patent; agonist activity for the V-2 receptor.