吡咯烷类生物碱新衍生物合成及解痉活性

Synthesis and Antispasmodic Activity of Pyrrolidine Alkaloid Derivatives

作者对吡咯烷类生物碱──红古豆碱及古豆碱进行化学结构改造，设计并合成了古豆醇酯类和红古豆醇酯类两个系列共九个新化合物，其中古豆醇酯类为具有解痉活性的新结构类型，各化学结构经ＩＲ，ＭＳ，１Ｈ－ＮＭＲ及元素分析确证．初步药理实验结果表明：所试验的衍生物（４～１１）均有不同程度的解痉活性，特别是衍生物（４～７）的活性高于市售抗胆碱药红古豆醇酯．

This paper reported pyrrolidine alkaloids-cuscohygrine and hygrine,which had no pharmacological activity and were modified in their strticttires.and it was recognized that more effective and selective derivatives were discovered.According to the cholinergic-receptor models and structure-activity relationshi.nine new derivatives of ester of cuscohygrinol and ester of hygrinol were designed and synthesized.Their chemical structures were indentified by IR,MS,1H-NMR elementary analysis.All the compounds have not been repored yet.The preliminary pharmacological results showed that compounds(4～11)had autispasmodic activity.The activities of compounds(4～7)were superior to that of ester of ctiscohygrinol,esperially.Further pharmacological tests will be performed.