Abstract
The synthesis and biological activity of sordarin oxazepine derivatives are described. The key step features a regioselective oxidation of an unprotected triol followed by double reductive amination to afford the ring-closed products. The spectrum of antifungal activity for these novel derivatives includes coverage of Candida albicans, Candida glabrata, and Cryptococcus neoformans.
MeSH terms
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Antifungal Agents / chemical synthesis*
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Antifungal Agents / pharmacology*
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Candida albicans / drug effects
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Candida glabrata / drug effects
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Cryptococcus neoformans / drug effects
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Fungi / drug effects*
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Hydrogen Bonding
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Indenes
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Microbial Sensitivity Tests
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Oxazepines / chemical synthesis*
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Oxazepines / pharmacology*
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Structure-Activity Relationship
Substances
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Antifungal Agents
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Indenes
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Oxazepines
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sordarin