Antimicrobial activity of some 1,2-benzisothiazoles having a benzenesulfonamide moiety.
Some sulfonamide and sulfonylurea derivatives of unsubstituted and 5-methylsubstituted 1,2-benzisothiazole were studied in vitro for their antimicrobial properties against bacteria and fungi. Compounds 7 and 8 exhibited good antibacterial activity against Gram positive bacteria. A strong synergism was observed when their growth-inhibitory effect was assayed in combination with trimethoprim by using Bacillus subtilis and Staphylococcus aureus as test microorganisms. The antimycotic action of benzenesulfonylurea derivative 9 was very marked for Madurella mycetomatis and dermatophytes Epidermophyton floccosum, Microsporum gypseum and Trichophyton spp.. Structure-activity relations are discussed.
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Dipartimento Farmaceutico, Via delle Scienze 78, 43100 Parma, Italy.
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D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D000892:Anti-Infective Agents, Urinary / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology; D004357:Drug Synergism; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000494:pharmacology*; D013453:Sulfonylurea Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D013844:Thiazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D014295:Trimethoprim / Q000494:pharmacology; D000096926:Benzenesulfonamides
D000900:Anti-Bacterial Agents; D000892:Anti-Infective Agents, Urinary; D000935:Antifungal Agents; D013449:Sulfonamides; D013453:Sulfonylurea Compounds; D013844:Thiazoles; D014295:Trimethoprim; D000096926:Benzenesulfonamides