C-terminal anthranoyl-anthranilic acid derivatives and their evaluation on CCK receptors.
A series of C-terminal anthranoyl-anthranilic acid derivatives arising from a strict bond disconnection approach of asperlicin were synthesized and examined for their CCK receptor affinities. These compounds represent the second step of our investigation directed toward the search for alternative substructures of asperlicin as a starting point for the development of a new class of CCK ligands. The obtained micromolar affinities for CCK-A rather than CCK-B receptor confirm that the anthranilic acid dimer represents a useful template for the development of selective CCK-A receptor ligands.
Varnavas
A
A
Department of Pharmaceutical Sciences, University of Trieste, Italy. varnavas@univ.trieste.it
Lassiani
L
L
Luxich
E
E
Valenta
V
V
D000818:Animals; D006168:Guinea Pigs; D008024:Ligands; D015394:Molecular Structure; D051381:Rats; D043886:Receptor, Cholecystokinin A; D043887:Receptor, Cholecystokinin B; D011949:Receptors, Cholecystokinin / Q000378:metabolism*; D062367:ortho-Aminobenzoates / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism*
D008024:Ligands; D043886:Receptor, Cholecystokinin A; D043887:Receptor, Cholecystokinin B; D011949:Receptors, Cholecystokinin; D062367:ortho-Aminobenzoates