Synthesis and antiulcer activity study of disubstituted alkyl 4-(substituted)-2,6- dimethyl-1-((4-oxo-3-(4-sulfamoylphenyl)-2- thioxo-3,4-dihydroquinazolin-1 (2H)-yl) methyl)-1,4-dihydropyridine-3,5 dicarboxylate

摘要

A 2-amino-N-(4-sulfamoyl phenyl) benzamide 1 has been prepared by reaction of anthranilic acid with sulfanilamide. Compound 1 with carbon disulphide furnish 4-(4-oxo-2-thioxo-l, 2-dihydroquinazolin-3(4H)-yl) benzene sulfonamide 2. The compound 2 on reaction with para formaldehyde and 1,4-dihydropyridine derivatives yields disubstituted alkyl 4-(substituted)-2,6-dimethyl-l-((4-oxo-3-(4-sulfamoyIphenyl)-2-thi-oxo-3,4-dihydroquinazolin-l(2H)-yl) methyl)-1,4-dihydropyri-dine-3,5 dicarboxylate 3a-h. Antiulcer activities of compounds 3a-h have been evaluated by estimating volume of gastric juice, total acidity, free acidity and ulcer index. Conjunction of 1,4-dihydropyridines with sulfanilamide and quinazolinone results in compounds with antiulcer activity comparable to that of ranitidine. Compounds substituted with methoxy and nitro groups exhibit maximum enhancement in activity.