SYNTHESIS AND BIOLOGICAL EVALUATION OF NEW 3-ARALKYLAMINO-2-ARYL-2H-1,2,4-PYRIDOTHIADIAZINE 1,1-DIOXIDES AS POTENTIAL CCK-RECEPTOR LIGANDS

A series of 2-aralkyl-4H-pyridothiadiazine 1,1-dioxides and kylamino-2 -aryl-2H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides structurally rel ated to quinazolinone CCK receptor antagonists were synthesized and ev aluated as CCK-A and CCK-B receptor ligands. The compounds were effect ive as cholecystokinin-ligands in the micromolar range of concentratio n, c.f. the cholecystokinin receptor antagonists asperlicin, lorglumid e or benzotript, and were thus less potent than the best quinazolinone s previously reported. Although the compounds were unsuitable for drug use, the work contributed to our understanding of the chemistry of un usual 2,3-disubstituted pyridothiadiazinedioxides.