Abstract A novel series of 4-(amino or acetamido)-N-{[3-(substituted aryl)-4-oxo-3, 4- dihydroquinazolin-2-yl]-methyl} benzenesulfonamide derivatives (1–19) were designed to assimilate 4-quinazolone and sulfonamide moieties in a single molecular framework. To derive entitled hybrid entities with structural diversity, an efficient multi-step synthetic approach initiated from glycine was developed, which involves milder conditions for ...