肉桂酰胺及α-苯基肉桂酰胺衍生物的合成及扩血管活性

SYNTHESIS AND VASODILATIVE ACTIVITIES OF CINNAMIDE AND α-PHENYLCINNAMIDE DERIVATIVES

摘要: 目的：寻找新型的抗高血压药物。方法：用典型的Knoevenagel缩合反应和混合酸酐法合成。结果：合成了9个肉桂酰胺类化合的和8个α-取代苯基肉桂酰胺类衍生物，均为新化合物。结论：体外扩血管活性试验表明，在分子的苯环与羰基间引入双键不利于化合物对去甲肾上腺素［以下简称NE］(10^-7 mol.L^-1)引起的大鼠主动脉条收缩抑制活性;在肉桂酰基的羰基α位引入大基团(取代苯环)可能有利于选择性地提高化合物对85.7 mmol.L^-1 KCl引起的大鼠主动脉条收缩的抑制作用。

Abstract: AIM: To search for compounds having strong vasodilating effect. METHODS: The classic Knoevenagel condensation and mixed anhydride method were used. RESULTS: Nine cinnamides and eight α-phenylcinnamide derivatives were synthesized. CONCLUSION: Vasodilative activity screening in vitro showed that the olefinic linkage inserted between the benzene ring and carbonyl group was unfavourable to the inhibiting activity on noradrenaline (10^-7 mol.L^-1) induced contraction of rat aortic strip, while the introduction of bulky groups (substituted phenyl) at α position of the cinnamoyl carbonyl group might selectively enhance the inhibiting activity against 85.7 mmol.L^-1 KCl induced contraction of rat aortic strip.