title: Sordarin oxazepine derivatives as potent antifungal agents.
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.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492, USA. michael.serrano-wu@bms.com
authors.forename: Michael H
authors.initials: MH
authors.lastname: Serrano-Wu
authors.forename: Denis R
authors.initials: DR
authors.lastname: St  Laurent
authors.forename: Yijun
authors.initials: Y
authors.lastname: Chen
authors.forename: Stella
authors.initials: S
authors.lastname: Huang
authors.forename: Kin-Ray
authors.initials: KR
authors.lastname: Lam
authors.forename: James A
authors.initials: JA
authors.lastname: Matson
authors.forename: Charles E
authors.initials: CE
authors.lastname: Mazzucco
authors.forename: Terry M
authors.initials: TM
authors.lastname: Stickle
authors.forename: Thomas P
authors.initials: TP
authors.lastname: Tully
authors.forename: Henry S
authors.initials: HS
authors.lastname: Wong
authors.forename: Dolatrai M
authors.initials: DM
authors.lastname: Vyas
authors.forename: Balu N
authors.initials: BN
authors.lastname: Balasubramanian
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects; D041221:Candida glabrata / Q000187:drug effects; D003455:Cryptococcus neoformans / Q000187:drug effects; D005658:Fungi / Q000187:drug effects*; D006860:Hydrogen Bonding; D007192:Indenes; D008826:Microbial Sensitivity Tests; D010077:Oxazepines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000935:Antifungal Agents; D007192:Indenes; D010077:Oxazepines; C003329:sordarin