Core-Modified Sordaricin Derivatives: Synthesis And Antifungal Activity

Core-modified sordaricin derivatives were prepared via biotransformation followed by chemical modification and tested for antifungal actin it. The antifungal activity proved to be very sensitive to modifications in the sterics and/or lipophilicity of the diterpene skeleton. Introduction of polar groups such as hydroxyl in the diterpene core results in loss of potency awhile small and lipophilic groups such Lis fluorine and the 7,8-olefin are well tolerated. (C) 2002 Elsevier Science Ltd. All rights reserved.