Biological studies on 1,2-benzisothiazole derivatives VI Antimicrobial activity of 1,2-benzisothiazole and 1,2-benzisothiazolin-3-one derivatives and of some corresponding 1,2-benzisoxazoles.
Numerous 1,2-benzisothiazole and 1,2-benzisothiazolin-3-one derivatives, variously substituted in the different positions of the molecule, were tested for their in vitro antimicrobial activity. Some corresponding 1,2-benzisoxazoles and 1,2-benzisoxazolin-3-ones were also considered. Several compounds possess a potent and broad antibacterial and antifungal activity, particularly against Gram positive microorganisms, yeasts and dermatophytes. 1,2-Benzisothiazolin-3-ones were found to be the most active substances. On the contrary, the benzisoxazoles and the benzisoxazolin-3-ones considered were devoid of activity. The results obtained are discussed on the basis of structure-activity relationships.
Zani
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F
Dipartimento Farmaceutico, Facoltà di Farmacia, Parma.
Mingiardi
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MR
Maggiali
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CA
Mazza
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P
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D005658:Fungi / Q000187:drug effects; D007555:Isoxazoles / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D007555:Isoxazoles; D013844:Thiazoles