Abstract
Thein vitro antifungal activity of several N2-phenyl-3(2H)-isothiazolones substituted at C4 of the phenyl moiety with heterocyclic nucleus or groups of different physico-chemical properties against four human pathogenic fungi was determined by broth macrodilution method; results were compared with those obtained with itraconazole and ketoconazole. These isothiazolones showed moderate to high activity against some or all tested strains and in comparison with the reference drugs, 5-chloro-2-(4-nitrophenyl)isothiazol-3-one (1g), 5-chloro-2-phenylisothiazol-3-one (1c), 4-[4-(5-chloro-3-oxo-3H-isothiazol-2-yl)phenyl]-1,4-dihydrotriazol-5-one (1s) and 2-(4-nitrophenyl)isothiazol-3-one (2g) againstAspergillus niger, 5-chloro-2-(4-nitrophenyl)isothiazol-3-one (1g) and 4-[4-(5-chloro-3-oxo-3H-isothiazol-2-yl)phenyl]piperazine-1-carboxamide (1q) againstTrichophyton mentagrophytes had comparable activity, compounds1g and2g showing higher activity againstMicrosporum canis. Antifungal activity was favored by the presence of chlorine at C5 of the isothiazolone and/or the presence of nitro group or heterocyclic nucleus at C4 of the phenyl ring and proper hydrophilicity of the molecule.
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Abbreviations
- MIC(s):
-
minimal inhibitory concentration(s)
- Mops:
-
3-morpholinopropanesulfonic acid
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Adibpour, N., Khalaj, A., Rezaee, S. et al. In Vitro antifungal activity of 2-(4-substituted phenyl)-3(2H)-isothiazolones. Folia Microbiol 52, 573–576 (2007). https://doi.org/10.1007/BF02932185
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DOI: https://doi.org/10.1007/BF02932185