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硫代氢化脲嘧啶的合成及其对Hill反应的抑制活性
Synthesis of Thiohydrouracils and Their Inhibitory Activity against Hill Reaction
【摘要】 为了寻找高活性的Hill反应抑制剂,以β-氨基丙酸为原料,经过四步反应,合成了一系列未经文献报道的3-取代硫代氢化脲嘧啶.所有新化合物的结构均经过1HNMR,IR和元素分析证.初步的生物活性测试表明,所合成的化合物能有效地抑制Hill反应,如化合物5j有很高的抑制活性(IC50=0.82μg?mL-1).
【Abstract】 In order to find highly active inhibitors of Hill reaction, a series of thiohydrouracil derivatives have been synthesized by a four-step synthetic route. The structures of all compounds were confirmed by elemental analysis, 1H NMR and IR spectra. Preliminary bioassay showed that these compounds could inhibit Hill reaction effectively, for example, compound 5j exhibited high inhibitory activity with IC50=0.82 μg?mL-1.
【基金】 国家重点基础研究发展规划(No.2003CB114400);国家自然科学基金(No.20372040);国家高等教育博士点基金资助项目.
- 【文献出处】 有机化学 ,Chinese Journal of Organic Chemistry , 编辑部邮箱 ,2005年07期
- 【分类号】TQ457.29
- 【被引频次】1
- 【下载频次】137