一枝蒿酮酸苄酯类衍生物的合成、体外抗流感病毒和单纯I, II型疱疹病毒活性研究

为了提高一枝蒿酮酸的生物活性, 以一枝蒿酮酸和取代苄醇为原料. 在偶联剂DCC/DMAP的作用下, 合成了10种一枝蒿酮酸苄酯衍生物2a～2j, 所合成的化合物均经过IR, 1H NMR, ESI-MS等分析方法进行了表征, 并对所合成的化合物2a～2j进行了初步的体外抗A, B型流感病毒和单纯I, II型疱疹病毒活性研究, 结果表明: 大部分化合物对A, B型流感病毒具有较强的抑制活性, 其中化合物2e抑制A3, B型流感病毒的IC50值分别为5.5, 5.5 μmol/L, 化合物2i抑制A型流感病毒IC50值为: 7.8 μmol/L, 化合物2e和2i可作为抗流感病毒的先导化合物; 大部分化合物在0.1 μg/mL浓度下对I, II型疱疹病毒具有显著的抑制活性．

Synthesis of Rupestonic Acid Benzyl Ester Derivatives and in vitro Anti Influenza Virus and Herpes Simplex Type I and II Viruses

To improve rupestonic acid biological activities, ten rupestonic acid benzyl ester derivatives were synthesized in the presence of DCC/DMAP with the rupestonic acid and substituted benzyl alcohol as starting materials. The synthesized compounds 2a～2j were confirmed by the methods of IR, 1H NMR, ESI-MS and preliminarily assayed in vitro against influenza viruses A3, B and herpes simplex virus I (HSV-I), herpes simplex virus II (HSV-II). The results showed that most of the synthesized compounds had distinct inhibition against influenza viruses, 2e exhibited in vitro inhibitory activity against both influenza A3 and B viruses with IC50 values of 5.5, 5.5 μmol/L, respectively, and 2i showed higher activity against in-fluenza A virus with an IC50 value of 7.8 μmol/L. Therefore, compounds 2e, 2i can be as lead compounds for anti-flu agent. Most of the compounds showed higher inhibition against HSV-I and HSV-II viruses at 0.1 μg/mL concentration.