双四氢呋喃木脂素Prinsepiol酰化衍生物的合成及其抑菌活性研究

Synthesis and antifungal activity of acyl derivatives of Prinsepiol

【目的】寻找具有农用生物活性的新型化合物或具有新结构的化合物。【方法】以Prinsepiol为原料，选择性地对其4，4’位羟基进行酰化反应，设计、合成Prinsepiol的酰化衍生物，采用核磁共振谱、红外光谱、高分辨质谱法对其结构进行鉴定，并测定了衍生物对番茄灰霉菌孢子萌发的抑制作用。【结果】合成了10个Prinsepiol酰化衍生物。在Prinsepiol4，4’位引入不同酰基后化合物的抑菌活性均有不同程度提高，其中4，4’-二异丁酰基衍生物和4，4′-二乙酰基衍生物的抑菌活性均较好，有效中浓度（EC50）分别为3．85和5．60mg／L，是Prinsepiol的6～8倍。【结论】Prinsepiol4，4’位与其生物活性关系密切。

[Objective] The study was done in search of novel compounds or structures with bioactivity. [Method] The acetylation to the 4,4＇ hydroxyls of Prinsepiol was done selectively. Ten acyl derivatives were obtained and their structures were confirmed by NMR, IR and HRMS. The inhibition effects of the ten acyl derivatives on the spore germination of Botrytis cirerea were determined. [Result] Ten acyl derivatives were synthesized. The acyl derivatives all exhibited higher inhibitory effect than prinsepiol,among which isobutyryl and diacetate derivatives exhibited highest activity with EC50 of 3. 85 mg/L and 5. 60 mg/L respectively. [Conclusion] It＇s found that the 4,4＇of Prinsepiol is clearly related to its bioactivity.