24,25-环亚胺酵母甾醇的合成及对甾醇甲基化转移酶的抑制作用

Synthesis of 24,25-epiminozymosterol and its inhibitory effect on the 24,25-sterol methyl transferase

为合理设计合成抗真菌药物，以酵母中的生物合成中间体酵母甾醇作为原料，与叠氨化碘（IN3）的作用经四氢铝锂（LiAIH4）还原合成生物合成抑制剂──24，25-环亚胺酵母甾醇。经体外酶分析证明，该化合物对酵母中甾醇24，25-甲基化转移酶有显著的抑制作用（Ki＝10nM）。

In order to design and synthesize zymosterol(antifungal agent),which is the intermediate in ergosterol biosynthesis in yeast was used as the material to synthesize 24,25-epiminozymosterol biosynthetic inhibitor by reacting with iolide azide(IN3) and reduced with LiAlH4.The synthesized compound was showed in vitro enzyme assay to have strong inhibitory effect on 24,25-sterol methyl transterase.