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Chin. J. Org. Chem. ›› 2008, Vol. 28 ›› Issue (10): 1807-1812. Previous Articles     Next Articles

Reports

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

雍建平a,b ; 阿吉艾克拜尔·艾萨*,a   

  1. (a中国科学院新疆理化技术研究所 乌鲁木齐 830011)
    (b 中国科学院研究生院 北京 100039)
  • 收稿日期:2008-02-28 修回日期:2008-04-20 发布日期:2008-10-20
  • 通讯作者: 阿吉艾克拜尔·艾萨*

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

YONG, Jian-Ping a,b; HAJI, Akber Aisa*,a   

  1. (a Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Science, Urumqi 830011)
    (b Graduate School of Chinese Academy of Science, Beijin 100039)
  • Received:2008-02-28 Revised:2008-04-20 Published:2008-10-20
  • Contact: HAJI, Akber Aisa*

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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 .

Key words: rupestonic acid amide derivative, synthesis, influenza A3, B virus, biological activity, herpes simplex virus