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对咖啡酸和阿魏酸的化学结构进行改造，得到两种肉桂酰胺类似物Ｎ３－（５－甲基异唑）基－３，４－二羟基肉桂酰胺（化合物１）和 Ｎ４－安替比林基－４－羟基－３－甲氧基肉桂酰胺（化合物２），并分别对其拮抗内皮素－１（ＥＴ－１）的缩血管及致血管平滑肌细胞增殖效应进行了初步研究。结果发现，这四种化合物对ＥＴ－１ 的缩血管及致血管平滑肌细胞增殖效应有明显的拮抗作用，该作用具剂量依赖性，经药效动力学分析，阿魏酸及其衍生物的拮抗活性显著大于咖啡酸及其衍生物；这四种化合物能剂量依赖性地抑制ＥＴ－１ 致血管平滑肌细胞增殖作用。咖啡酸和阿魏酸及其衍生物为一类新的ＥＴ 拮抗剂
The chemical structure of caffeic acid and ferulic acid was modified to give two cinnamide analogs, N3- (5-methylisoxazolyl) -3,4-dihydroxycinnamide (Compound 1) and N4- 4-hydroxy-3-methoxycinnamic acid amide (compound 2) was used in this study. The inhibitory effects on endothelin-1 (ET-1) vasoconstriction and the proliferation of vascular smooth muscle cells were studied. The results showed that these four compounds have a significant antagonistic effect on the proliferation of vascular smooth muscle cells and vasoconstriction of ET-1 in a dose-dependent manner. The antagonistic effects of ferulic acid and its derivatives Activity significantly greater than caffeic acid and its derivatives; these four compounds can inhibit ET-1-induced vascular smooth muscle cell proliferation in a dose-dependent manner. Caffeic acid and ferulic acid and their derivatives are a new class of ET antagonists