Novel and efficient synthesis and antifungal evaluation of 2,3-functionalized cholestane and androstane derivatives

作者：Jursic Branko S; Upadhyay Sunil Kumar; Creech Clinton C; Neumann Donna M^*

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(24): 7372-7375.

DOI：10.1016/j.bmcl.2010.10.044

• Androstane
• Cholestane
• Succinic esters
• Antifungal steroids
• Dihydroxy steroids

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.

• 出版日期2010-12-15