Chin. J. Org. Chem. ›› 2014, Vol. 34 ›› Issue (5): 973-979.DOI: 10.6023/cjoc201312003 Previous Articles     Next Articles



梁光平a,b, 曹佩雪a, 杨秀虾a,b, 黄正明c, 刘青川c, 梁光义a, 徐必学a   

  1. a 贵州省中国科学院天然产物化学重点实验室 贵阳 550002;
    b 贵阳中医学院 贵阳 550002;
    c 中国人民解放军第三○二医院 北京 100039
  • 收稿日期:2013-12-02 修回日期:2014-01-03 发布日期:2014-01-03
  • 通讯作者: 梁光义,徐必学;
  • 基金资助:

    国家自然科学基金(No. 81360472)、贵阳中医学院研究生教育创新计划(No. ZYYCX12018)资助项目.

Synthesis and Anti-hepatitis B Virus Activities of Nitric Oxide-Releasing Derivatives of Matijin-Su

Liang Guangpinga,b, Cao Peixuea, Yang Xiuxiaa,b, Huang Zhengmingc, Liu Qingchuanc, Liang Guangyia, Xu Bixuea   

  1. a Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, Guiyang 550002;
    b Guiyang College of Traditional Chinese Medicine, Guiyang 550002;
    c 302 Hospital of PLA, Beijing 100039
  • Received:2013-12-02 Revised:2014-01-03 Published:2014-01-03
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 81360472), and the Graduate Education Innovation Project of Guiyang College of Traditional Chinese Medicine (No. ZYYCX12018).

By using N-(N-benzoyl-L-phenylalanyl)-O-acetyl-L-phenylalanol, named Matijin-Su, as a lead compound, a series of nitric oxide-releasing derivatives of Matijin-Su were synthesized and evaluated for their anti-hepatitis B virus activities in HepG2 2.2.15 cells. Compounds 6d, 6e and 6g exhibited significant anti-HBV activities. The 50% inhibitory concentrations of these compounds towards HepG2 2.2.15 cells were 6.88, 37.51 and 11.07 μmol/L. Compounds 6d and 6g were less than Matijin-Su (IC50: 11.16 μmol/L). Compound 6d has potent in vitro anti-HBV activity, and could be worth of further research.

Key words: derivatives of Matijin-Su, nitric oxide donor, synthesis, anti-hepatitis B virus activity