Antimicrobial and genotoxic activities of N-(2-hydroxyethyl)-1,2-benzisothiazol-3(2H)-thione carbamic esters.
The antimicrobial properties of N-(2-hydroxyethyl)-1,2-benzisothiazol-3(2H)-thione (1a,b) and its carbamic esters 2a,b-6a,b were tested in vitro against Gram positive and Gram negative bacteria, yeasts and dermatophytes. All compounds markedly inhibit the growth of Gram positive bacteria exhibiting MIC values ranging from 1.25 to 10 micrograms/ml. A strong antifungal activity is exerted against dermatophytes with MICs, in general, between 0.7 and 12 micrograms/ml. Structure-activity relationship studies show that these compounds are, in most cases, more effective than the corresponding benzisothiazolone analogues 7-12. None of the tested compounds shows genotoxic properties by Bacillus subtilis rec-assay and Salmonella-microsome test.
Zani
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Dipartimento Farmaceutico, Università degli Studi, Parma, Italy.
Pregnolato
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Zampollo
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D000900:Anti-Bacterial Agents / Q000494:pharmacology* / Q000633:toxicity; D002219:Carbamates / Q000494:pharmacology* / Q000633:toxicity; D004247:DNA / Q000187:drug effects; D004249:DNA Damage; D008826:Microbial Sensitivity Tests; D009152:Mutagenicity Tests; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000494:pharmacology* / Q000633:toxicity
D000900:Anti-Bacterial Agents; D002219:Carbamates; D013844:Thiazoles; D004247:DNA