一枝蒿酮酸酰胺衍生物的合成和抗A3, B型流感病毒和 单纯I, II型疱疹病毒活性研究

从新疆一枝蒿中分离得到了单体化合物一枝蒿酮酸, 然后以一枝蒿酮酸和有机胺为原料, 在偶联剂DCC, HOBt/DMAP的作用下, 合成了13种未见文献报道的一枝蒿酮酸酰胺衍生物2a～2m. 所合成的化合物经过IR, 1H NMR, ESI-MS等分析方法进行了表征, 并对化合物2a～2m进行初步的体外抗A3, B型流感病毒和单纯I, II型疱疹病毒活性研究. 初步试验结果表明化合物2a同时具有抗A3, B型流感病毒活性, 而且抗B型流感病毒活性比母体化合物的活性较高. 化合物2d的抗B型流感病毒活性比母体化合物高16倍, 化合物2e同时具有较强的抗单纯I, II型疱疹病毒活性.

Synthesis of Rupestonic Acid Amide Derivatives and in vitro Anti-influenza A3, B and Herpes Simplex Type I and II Viruses

The rupestonic acid (compound 1) was isolated from the Chinese herbal medicine Artemisia rupestris L. (its Chinese name being Yizhihao). Then, 13 rupestonic acid amide derivatives 2a～2m were synthesized using rupestonic acid and organic amines in the presence of DCC, HOBt/DMAP and their structures were comfirmed by the methods of IR, 1HNMR, and ESI-MS. All compounds were preliminarily assayed in vitro against influenza A3, B, herpes simplex I (HSV-I) and herpes simplex II (HSV-II) viruses, showing that 2a was inhibitive to both influenza A3 and B viruses, and had the higher inhibition against influenza B virus than the parent compound 1. The inhibition of 2d against influenza B virus was 16-fold higher than that of the parent compound and 2e was more active both to HSV-I and HSV-II viruses .