Simple synthesis of novel diphenylsulfapyrimidine acetates from chalcones and their antimicrobial activity.
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.
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Chemistry Department, Faculty of Science, Benha University, Benha, Egypt.
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D000085:Acetates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002599:Chalcone / Q000737:chemistry*; D005658:Fungi / Q000187:drug effects; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013414:Sulfaguanidine / Q000737:chemistry; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000085:Acetates; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D011743:Pyrimidines; D013449:Sulfonamides; D013414:Sulfaguanidine; D002599:Chalcone