Abstract
New linear and cyclic guanidines were synthesized and tested in vitro for their antifungal activity toward clinically relevant strains of Candida species, in comparison to fluconazole. Macrocyclic compounds showed a minimum inhibitory concentration in the micromolar range and a biological activity profile in some cases better than that of fluconazole. One macrocyclic derivative was also tested against Aspergillus species and showed high antifungal activity comparable to that of amphotericin B and itraconazole.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antifungal Agents / chemical synthesis
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Antifungal Agents / chemistry
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Antifungal Agents / pharmacology
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Aspergillus / drug effects*
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Candida / drug effects*
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Drug Design
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Guanidine / analogs & derivatives*
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Guanidine / chemical synthesis
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Guanidine / chemistry
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Guanidine / pharmacology
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Humans
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Macrocyclic Compounds / chemical synthesis*
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Macrocyclic Compounds / chemistry
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Macrocyclic Compounds / pharmacology*
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Microbial Sensitivity Tests
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Urea / analogs & derivatives*
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Urea / chemical synthesis
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Urea / chemistry
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Urea / pharmacology
Substances
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Antifungal Agents
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Macrocyclic Compounds
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guanidine carboxamide
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Urea
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Guanidine