为了提高一枝蒿酮酸的生物活性, 以一枝蒿酮酸和3-取代苯基-5-氨甲基-异噁唑为原料, 在偶合试剂DCC,HOBt/ DMAP 的作用下, 合成了6 个未见文献报道的含异噁唑的一枝蒿酮酸酰胺衍生物3a～3f. 所合成的化合物均经过IR, 1H NMR, 13C NMR, ESI-MS 等分析方法表征及初步体外抗A (H3N2, H1N1)型和B 型流感病毒活性研究. 初步实验结果表明: 化合物3c 同时具有抗A (H3N2)型和B 型流感病毒活性, 化合物3c 和3e 表现出比母体化合物强的抗B型流感病毒活性.
To improve biological activity of rupestonic acid, six rupestonic acid amide derivatives containing isoxazole were synthesized in the presence of DCC, HOBt/DMAP using the rupestonic acid and 3-aryl-5-isoxazole-methylamine as the starting materials. The synthesized compounds 3a～3f were confirmed by the methods of 1H NMR, 13C NMR, IR, ESI-MS techniques and preliminarily assayed in vitro against influenza viruses A and B. The results showed that compound 3c showed better activity against both influenza viruses A (H3N2) and B, and compounds 3c and 3e had the higher inhibition against influenza B virus than the parent compound 1.
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