Chin. J. Org. Chem. ›› 2019, Vol. 39 ›› Issue (9): 2574-2580.DOI: 10.6023/cjoc201901016 Previous Articles     Next Articles

ARTICLE

白杨素衍生物的合成及体外抗弓形虫活性研究

尚凡凡, 金澜, 张海滨, 朴莲荀, 全哲山   

  1. 延边大学药学院 延吉 133002
  • 收稿日期:2019-01-11 修回日期:2019-02-28 出版日期:2019-09-25 发布日期:2019-03-21
  • 通讯作者: 朴莲荀, 全哲山 E-mail:zsquan@ybu.edu.cn;lxpiao@ybu.edu.cn
  • 基金资助:

    国家自然科学基金(Nos.21662036,81660344)资助项目.

Synthesis and Anti-toxoplasma Activity in Vitro of Chrysin Derivatives

Shang Fanfan, Jin Lan, Zhang Haibin, Piao Lianxun, Quan Zheshan   

  1. College of Pharmacy, Yanbian University, Yanji 133002
  • Received:2019-01-11 Revised:2019-02-28 Online:2019-09-25 Published:2019-03-21
  • Contact: 10.6023/cjoc201901016 E-mail:zsquan@ybu.edu.cn;lxpiao@ybu.edu.cn
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 21662036, 81660344).

In this paper, 18 novel chrysin derivatives were designed and synthesized. All target compounds were tested for anti-Toxoplasma activity by methyl thiazolyl tetrazolium (MTT) colorimetric method. The chemical structures were characterized by 1H NMR, 13C NMR and HRMS spectra. The selectivity index of 5-hydroxy-7-methoxy-4-oxo-N,2-diphenyl-4H-chro-mene-8-sulfonamide (D2) was 1.76, indicating that the anti-toxoplasma activity of compound D2 was significantly higher than that of the lead compound chrysin and the positive control drug sulfadiazine.

Key words: chrysin derivatives, synthesis, toxoplasma activity, in vitro, selectivity index