咪唑芳酸衍生物的合成及抗血小板聚集活性

    Synthesis of Imidazole-Aromatic Acid Derivatives and Their Inhibitory Effect on Platelet Aggregation

    • 摘要: 合成4个咪唑芳酸衍生物。方法 以香草酸、丁香酸为起始原料,经Williamson醚化、亲核取代和水解反应,合成咪唑芳酸衍生物4 a~4 d。结果 目标化合物的结构经IR、1H-NMR、13C-NMR及MS确证。结论 初步的药理实验结果显示,在12 mmol·L-1浓度下,化合物4 a的血小板抑制率达到84.5%。

       

      Abstract: OBJECTIVE To synthesize four new compounds of imidazole-aromatic acid derivatives. METHODS Imidazole-aromatic acid derivatives were prepared from vanillic acid, syringic acid via Williamson etherification, nucleophilic substitution, and hydroxylation. RESULTS The structures of the target compounds were confirmed by IR, 1H-NMR, 13C-NMR and MS. CONCLUSION Preliminary pharmacological results showed that the inhibitory effect on platelet aggregation of compound 4a at 12 mmol·L-1 was 84.5%.

       

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