Abstract A series of 2-aralkyl-4H-pyridothiadiazine 1, 1-dioxides and 3-aralkylamino-2-aryl- 2H-pyrido [4, 3-e]-1, 2, 4-thiadiazine 1, 1-dioxides structurally related to quinazolinone CCK receptor antagonists were synthesized and evaluated as CCK-A and CCK-B receptor ligands.