摘要/Abstract

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


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