Abstract
A series of novel triazol-3-ones have been synthesized, and their in vitro and in vivo antifungal properties are reported. Compound 68 (itraconazole), which displays a pronounced oral activity against vaginal candidosis in rats and against microsporosis in guinea pigs, has been selected for clinical evaluation.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antifungal Agents / chemical synthesis*
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Aspergillus fumigatus / drug effects
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Candida / drug effects
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Candidiasis, Vulvovaginal / drug therapy
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Cryptococcus neoformans / drug effects
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Dermatomycoses / drug therapy
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Female
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Guinea Pigs
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Itraconazole
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Ketoconazole / analogs & derivatives*
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Ketoconazole / chemical synthesis
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Ketoconazole / therapeutic use
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Microsporum / drug effects
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Phialophora / drug effects
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Rats
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Rats, Inbred Strains
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Sporothrix / drug effects
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Triazoles / chemical synthesis*
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Triazoles / therapeutic use
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Trichophyton / drug effects
Substances
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Antifungal Agents
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Triazoles
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Itraconazole
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Ketoconazole