title: Synthesis of N-terminal substituted anthranilic acid dimer derivatives for evaluation on CCK receptors.
abstract: 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.
authors.affiliation: Department of Pharmaceutical Sciences, University of Trieste, Italy. varnavas@univ.trieste.it
authors.forename: A
authors.initials: A
authors.lastname: Varnavas
authors.forename: V
authors.initials: V
authors.lastname: Valenta
authors.forename: F
authors.initials: F
authors.lastname: Berti
authors.forename: L
authors.initials: L
authors.lastname: Lassiani
mesh_terms: D000818:Animals; D001570:Benzodiazepinones / Q000494:pharmacology; D019281:Dimerization; D006168:Guinea Pigs; D008958:Models, Molecular; D051381:Rats; D011949:Receptors, Cholecystokinin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D062367:ortho-Aminobenzoates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D001570:Benzodiazepinones; D011949:Receptors, Cholecystokinin; D062367:ortho-Aminobenzoates; C046367:asperlicin