A series of new N-substituted anthranilic acid dimer derivatives having a C-terminal Phe residue was synthesized and evaluated
for their affinity for CCK receptors. These compounds resulted from a blended approach based firstly on the use of an alternative
substructure embedded within asperlicin and secondly on the derivatization of this template with substituents chosen considering
the C-terminal primary structure of the endogenous ligand. Although these compounds exhibited a regnylogical-type organization
similar to that of CCK-4, they are characterized by about 1000-fold greater affinity for CCK-A receptor than the C-terminal
tetrapeptide.
