有机化学 ›› 2019, Vol. 39 ›› Issue (9): 2574-2580.DOI: 10.6023/cjoc201901016 上一篇    下一篇

研究论文

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).

设计并合成了18个未见报道的白杨素类衍生物,采用噻唑蓝(MTT)比色法对所有化合物进行体外抗弓形虫活性测定,其化学结构均经过1H NMR,13C NMR以及HRMS的联合确证.结果显示,7-甲氧基-8-(NN-双(二乙羟基)-磺酰胺基)-白杨素(D2)的选择性指数为1.76,其抗弓形虫活性明显强于先导化合物白杨素及阳性对照药磺胺嘧啶,具有深入的研究价值.

关键词: 白杨素类衍生物, 合成, 抗弓形虫活性, 体外, 选择性指数

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