白杨素衍生物的合成及体外抗弓形虫活性研究
收稿日期: 2019-01-11
修回日期: 2019-02-28
网络出版日期: 2019-03-21
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
Received date: 2019-01-11
Revised date: 2019-02-28
Online published: 2019-03-21
Supported by
Project supported by the National Natural Science Foundation of China (Nos. 21662036, 81660344).
尚凡凡 , 金澜 , 张海滨 , 朴莲荀 , 全哲山 . 白杨素衍生物的合成及体外抗弓形虫活性研究[J]. 有机化学, 2019 , 39(9) : 2574 -2580 . DOI: 10.6023/cjoc201901016
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
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