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有机化学
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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 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 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).

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补充材料

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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-（N，N-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