新型齐墩果酸烟酸衍生物的合成及其活性研究

Study on the Conjugates of Oleanolic Acid-nicotinic Acid as Glycogen Phosphorylase Inhibitor

以五环三萜化合物齐墩果酸以及烟酸为原料,经取代、酯化、酰化、还原等反应合成了2个新型齐墩果酸烟酸衍生物,并对两个化合物进行了糖原磷酸化酶抑制活性测试。结果表明两个化合物均显示出了一定的糖原磷酸化酶抑制活性。此外,实验过程中,对齐墩果酸苄酯的酯化反应进行了优化。中间体及目标产物的结构均经NMR、IR和MS确证。

Two novel conjugates of oleanolic acid-nicotinic acid were synthesized by alkyl substitution,esterification,acylation and reduction reactions,etc. The results indicated that two derivatives exhibited some activities against glycogen phosphorylase. In addition,the esterification reaction at C-3 position of oleanolic acid benzyl ester was optimized during the experimental process. The structure of intermediates and target product were identified by IR,NMR and MS.