Simple synthesis of novel diphenylsulfapyrimidine acetates from chalcones and their antimicrobial activity.
ABSTRACT Given the significant low yield (19-43%) in reported results on the cyclocondensation of sulfaguanidine acetate with chalcones, a careful reinvestigation was carried out. A new series of chalcones, bearing electron-attracting groups in the aromatic moiety, have been used as precursors in the synthesis of diphenylsulfapyrimidine acetates with good yield. All synthesized compounds were active against G(+)- and G(-)-bacteria, and fungi. Combination of substituents (Cl, OMe, NO2, etc.) enhanced antimicrobial activity. Derivative with two NO2 groups exhibits an activity comparable with sulfadiazine.