Synthesis of antitrypanosomal 1,2-dioxane derivatives based on a natural product scaffold.
Synthesis of antitrypanosomal 1,2-dioxane derivatives based on a natural product scaffold.
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DOI：
10.1016/j.bmcl.2011.06.059
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发表时间：
2011-08-15
影响因子：
2.7
通讯作者：
Quinn, Ronald J.
中科院分区：
文献类型：
--
作者：
Holla, Harish;Labaied, Mehdi;Ngoc Pham;Jenkins, Ian D.;Stuart, Kenneth;Quinn, Ronald J.
A short practical synthesis of a new natural product based scaffold (6), based on antitrypanosomal and antimalarial compounds isolated from different Plakortis species is described. The scaffold contains a peroxide unit that is surprisingly stable to chemical manipulation elsewhere in the molecule, enabling it to be elaborated into a small library of derivatives. It is stable to ozonolysis, reductive work-up with dimethylsulfide and the Wittig reaction with stabilized phosphorus ylides. The scaffold along with its Wittig analogues has displayed low to sub-micro molar (0.2-3.3 μM) antitrypanosomal activity.
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