桂皮酰基取代的γ－氨基丁酸衍生物的合成及抗惊活性  

STUDIES ON SYNTHESIS AND ANTICONVULSANT-ACTIVITY OF CINNAMOYL γ-AMINO BUTYRIC ACID DERIVATIVES

作　　者：许凤荣[1] 王书玉[1] 

机构地区：[1]北京医科大学药学院

出　　处：《中国药物化学杂志》1994年第4期245-251,共7页Chinese Journal of Medicinal Chemistry

摘　　要：由芳香醛与丙二酸反应形成的桂皮酸衍生物，再与γ－氨基丁酸乙酯缩合成芳环取代的桂皮酰γ－氨基丁酸乙酯，该物先后经水解、胺解可得一系列桂皮酰γ－氨基丁酰胺类化合物。本文报道应用此法合成了１６个芳环取代的桂皮酰γ－氨基丁酰胺类化合物。以最大电休克法（ＭＥＳ）的动物模型进行抗癫痫实验筛选，发现它们均无或仅有弱的抗惊厥活性。Cinnamic acid derivatives obtained from aromatic aldehydes and malonic acid were used to condensate with ethyl ester of γ-amino butyric acid to get ethyl esters of substituted cinnamoyl-γ-aminobutyric acid.The latter compounds were converted into a series of cinnamoly γ-amino butyramide by hydrolysis and then aminolysis.By this method sixteen substituted phenyl cinnamoyl γ-aminobutyramides were synthesized.The anticonvulsant activity(maximal electroshock seizure,MES)of these compounds were tested.The results of animal experiments showed that they were all inactive or only possessed weak anticonvulsant activity.

关 键 词：桂皮酰胺类 化合物 Γ-氨基丁酸 抗惊厥药 

分 类 号：TQ464.7[化学工程—制药化工] R971.6[医药卫生—药品]