Pyridothiadiazinedioxides structurally related to quinazolinones cholecystokinin gastrin receptor ligands: synthesis and biological evaluation

The synthesis of 3-aralkyl-4-aryl-4H-, 3-aralkylamino-4-aryl-4H- and 3-aral kylsulfanyl-4-aryl-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides is descr ibed. Moreover, the affinity of the different compounds towards the cholecy stokinin CCK-A and CCK-B receptors was evaluated. For selected compounds, a ffinity on the two receptor subtypes was expressed in the micromolar range. This was comparable to the affinity observed with the naturally occurring CCK receptor antagonist asperlicin. (C) 1998 Elsevier Science B.V. All righ ts reserved.