Department of Chemistry, University of New Orleans, New Orleans, LA 70148, USA.
Bioorg Med Chem Lett. 2010 Dec 15;20(24):7372-5. doi: 10.1016/j.bmcl.2010.10.044. Epub 2010 Oct 14.
Synthetic modifications of cholesterol and other traditional steroid molecules have become a promising area for the exploration and development of novel antifungal agents, especially with respect to the development of fatty-acid esters of steroids. In addition, 2,3-functionalized steroids are also compounds with potentially interesting biological properties and proper functionalization of 2,3-steroids can lead to the development of efficient syntheses of building blocks for novel fatty-acid esters of steroids. In this Letter, we outline a novel and efficient approach to the synthesis of 2,3-functionalized cholestane and androstane derivatives and present their promising preliminary antifungal activities against a number of fungal species.
胆固醇和其他传统甾体分子的合成修饰已成为探索和开发新型抗真菌药物的一个有前途的领域，特别是在甾体脂肪酸酯的开发方面。此外，2,3-官能化甾体也是具有潜在有趣生物性质的化合物，2,3-甾体的适当官能化可以导致新型甾体脂肪酸酯的构建块的高效合成。在这封信中，我们概述了一种新颖且高效的方法来合成 2,3-官能化的胆甾烷和雄烷衍生物，并展示了它们对多种真菌物种具有有前途的初步抗真菌活性。
