1. Sordarin Oxazepine Derivatives as Potent Antifungal Agents
- Author
-
Kin-Ray Lam, Denis R. St. Laurent, Balu Balasubramanian, Dolatrai M. Vyas, Michael H. Serrano-Wu, H. Wong, Charles E. Mazzucco, Yijun Chen, Thomas P. Tully, Terry M. Stickle, Stella Huang, and James A. Matson
- Subjects
Antifungal Agents ,Stereochemistry ,Clinical Biochemistry ,Pharmaceutical Science ,Candida glabrata ,Microbial Sensitivity Tests ,Biochemistry ,Chemical synthesis ,Reductive amination ,Structure-Activity Relationship ,chemistry.chemical_compound ,Candida albicans ,Drug Discovery ,Molecular Biology ,Cryptococcus neoformans ,biology ,Organic Chemistry ,Fungi ,Hydrogen Bonding ,Biological activity ,biology.organism_classification ,Oxazepines ,Indenes ,chemistry ,Molecular Medicine ,Oxazepine ,Triol - 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