Chin. J. Org. Chem. ›› 2012, Vol. 32 ›› Issue (02): 333-337 .DOI: 10.6023/cjoc1108081 Previous Articles     Next Articles

Articles

新型一枝蒿酮酸异噁唑衍生物的合成及其抗A, B 型流感病毒活性研究

赵江瑜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 干旱区植物资源化学重点实验室 乌鲁木齐 830011;
    b 中国科学院研究生院 北京 100039
  • 收稿日期:2011-08-08 修回日期:2011-09-14 发布日期:2012-03-09
  • 通讯作者: 阿吉艾克拜尔·艾萨 E-mail:haji@ms.xjb.ac.cn
  • 基金资助:

    新疆自治区高技术研究发展计划(No. 200910105)、国家自然科学基金(No. 20872174)和国家杰出青年基金科学(No. 30925045)资助项目.

Synthesis of Novel Isoxazole Contained Rupestonic Acid Derivatives and in vitro Inhibitory Activity against Influenza Viruses A and B

Zhao Jiangyua,b, Aisa Hajia   

  1. a Key Laboratory of Chemistry of Plant Resources in Arid Region, Xinjiang Technical Institute of Physics and Chemistry,Chinese Academy of Sciences, Urumqi 830011;
    b Graduate School of Chinese Academy of Sciences, Beijing 100039
  • Received:2011-08-08 Revised:2011-09-14 Published:2012-03-09
  • Supported by:

    Project supported by the High-tech Research and Development Program of Xinjiang (No. 200910105), the National Natural Science Foundation of China (No. 20872174) and the China National Science Fund for Distinguished Young Scholars (No. 30925045).

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 3a3f 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.

Key words: rupestonic acid, isoxazole derivative, influenza virus, inhibitory activity