A water soluble benzazepine cholecystokinin-B receptor antagonist

Abstract A series of 5-substituted-3-ureidobenzazepin-2-ones bearing ioizable functionality was synthesized as potential cholecystokinin-B (CCK-B) receptor antagonists. SAR of this series of compounds demonstrated the optimal combination of a carboxylic acid and 5-cyclohexyl group, providing the high affinity (CCK-B IC 50 = 0.10 nM), water soluble CCK-B antagonist 2 .