Synthesis of conformationally constrained macrocyclic analogs of the potent and selective CCK-B antagonist CI-988

Article abstract of DOI:10.1016/S0040-4020(01)86257-8

A series of conformationally constrained analogs of the potent CCK-B antagonist CI-988 were prepared and evaluated for their CCK-B binding affinity. A macrolactamization reaction leading to the conformation of 11 to 14-membered rings was also investigated