索拉菌素恶唑嗪衍生物作为强效抗真菌剂。
Sordarin oxazepine derivatives as potent antifungal agents.
作者信息
Serrano-Wu Michael H, St Laurent Denis R, Chen Yijun, Huang Stella, Lam Kin-Ray, Matson James A, Mazzucco Charles E, Stickle Terry M, Tully Thomas P, Wong Henry S, Vyas Dolatrai M, Balasubramanian Balu N
机构信息
Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492, USA.
出版信息
Bioorg Med Chem Lett. 2002 Oct 7;12(19):2757-60. doi: 10.1016/s0960-894x(02)00529-2.
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.
描述了索拉菌素恶唑嗪衍生物的合成及其生物活性。关键步骤的特点是对未保护的三醇进行区域选择性氧化，然后进行双还原胺化反应以得到闭环产物。这些新型衍生物的抗真菌活性谱涵盖白色念珠菌、光滑念珠菌和新型隐球菌。
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