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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](10-7mol·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857mmol·L-1KCl引起的大鼠主动脉条收缩的抑制作用
Objective: To search for new antihypertensive drugs. Method: Synthesis using a typical Knoevenagel condensation reaction and mixed anhydride method. RESULTS: Nine cinnamamide-based compounds and eight α-substituted phenylcinnamic acid derivatives were synthesized and all were novel compounds. CONCLUSION: In vitro vasodilating activity assays show that the introduction of double bonds between the benzene ring and the carbonyl of the molecule is not conducive to the compound’s contraction of rat aortic strips caused by noradrenaline [hereinafter referred to as NE] (10-7 mol·L-1). Inhibitory activity; the introduction of a large group (substituted phenyl ring) at the carbonyl alpha position of cinnamoyl moieties may be beneficial to selectively increase the inhibitory effect of the compound on the contraction of rat aorta strips induced by 857mmol·L-1KCl.