芳酰胺及肉桂酰胺类衍生物的合成及扩血管活性

SYNTHESIS AND VASODILATING ACTIVITY OF BENZAMIDE AND CINNAMIDE DERIVATIVES

摘要: 目的：寻找新型的抗高血压药物。方法：用混合酸酐法合成。结果：合成了20个芳酰胺类（I）和肉桂酰胺类（II）衍生物。结论：药理筛选表明，部分化合物对去甲肾上腺素（10^-7 mol.L^-1）引起的大鼠主动脉条收缩有较好的抑制作用，其中化合物I₅的钾离子开放活性与尼可地尔（nicorandil）相当，化合物II8显示有钙离子通道拮抗活性，并有较强的扩血管活性。

Abstract: AIM: To search for compounds having strong vasodilating effect. METHODS: The mixed anhydride method was used. RESULTS: Twenty benzamides(I_1～12) and cinnamides(II_1～8) were designed and synthesized. CONCLUSION: All synthesized amides were submitted to pharmacological screening and 0.1 μmol.L^-1 (10-7mol.L^-1) noradrenaline induced contraction of rat aortic strip was taken as criterion. Compound I₅ was shown to be a potent potassium channel activator. Compound II₈ exhibited calcium antagonistic activity and showed potent vasodilating activity.