Benzotriazonine as a new core structure for the design of CCK-receptor antagonists

The search for heterocyclic scaffolds for the design of non-peptidic and highly selective agonists or antagonists of peptide hormone receptors led to 4-N-benzyl-2,3,4,5,6,7-hexahydro-1H-1,4,7-benzotriazonin-2, 6-dione with a 9-membered core structure as a new low mass lead compound that exhibits submicromolar antagonistic activity at the CCK-A receptor with a 54-fold selectivity over the CCK-B/gastrin receptor.