1. Sordarin oxazepine derivatives as potent antifungal agents.
- Author
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Serrano-Wu MH, St Laurent DR, Chen Y, Huang S, Lam KR, Matson JA, Mazzucco CE, Stickle TM, Tully TP, Wong HS, Vyas DM, and Balasubramanian BN
- Subjects
- Candida albicans drug effects, Candida glabrata drug effects, Cryptococcus neoformans drug effects, Hydrogen Bonding, Indenes, Microbial Sensitivity Tests, Structure-Activity Relationship, Antifungal Agents chemical synthesis, Antifungal Agents pharmacology, Fungi drug effects, Oxazepines chemical synthesis, Oxazepines pharmacology
- 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.
- Published
- 2002
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