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 hi ghly 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 subm icromolar antagonistic activity at the CCK-A receptor with a 54-fold select ivity over the CCK-B/gastrin receptor. Copyright (C) 1999 European Peptide Society and John Wiley & Sons, Ltd.