Structure-activity relationships of non-peptide vasopressin V1a antagonists: 1-(1-multi-substituted benzoyl 4-piperidyl)-3,4-dihydro-2(1H)-quinolinones.

During our systematic studies on the arginine vasopressin receptor V-1a-antagonistic activity of 1-(1-benzoyl substituted 4-piperidyl)-3,4-dihydro-2(1H)-quinolinones, we found a general substituent effect on the benzene ring, Hydrogen-bonding ability at the ortho position was especially important for enhancement of the affinity of multi-substituted analogs, Details of the syntheses and structure-activity relationships for this series are presented.