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有机化学
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有机化学 ›› 2010, Vol. 30 ›› Issue (05): 691-697. 上一篇    下一篇

研究论文

5-(4-羟基苯基)-2,4-咪唑啉二酮酯类化合物的合成及其生物活性

韩金涛，王进敏，陈守聪，邱立红，王明安*   

  1. (中国农业大学应用化学系 北京 100193)
  • 收稿日期:2009-07-31 修回日期:2009-11-05 发布日期:2009-12-07
  • 通讯作者: 王明安 E-mail:wangma@cau.edu.cn, wangmingan2003@yahoo.com
  • 基金资助:

    国家级.国家自然科学基金

Synthesis and Biological Activities of 5-(4-Hydroxyphenyl)- 2,4-imidazolidinedione Esters

HAN Jin-Tao, WANG Jin-Min, CHEN Shou-Cong, QIU Li-Hong, WANG Ming-An   

  1. (Department of Applied Chemistry, China Agricultural University, Beijing 100193)
  • Received:2009-07-31 Revised:2009-11-05 Published:2009-12-07

PDF

1236

被引次数

17

在模拟AdSS酶天然抑制剂结构合成5-(4-羟基苄基)-2,4-咪唑啉二酮酯系列化合物的基础上, 为优化其结构,以5-(4-羟基苯基)-2,4-咪唑啉二酮为中间体, 合成了28个未见文献报道的5-(4-羟基苯基)-2,4-咪唑啉二酮羧酸酯类化合物, 它们的结构均经IR, 1H NMR和元素分析表征. 初步生物活性测试表明目标化合物5-(4-羟基苯基)-2,4-咪唑啉二酮对叔丁基苯甲酸酯(2i)和2-噻吩酸酯(3b)在浓度200 (g/mL时对拟南芥生长抑制率达70%.

关键词: AdSS酶抑制剂, 5-(4-羟基苯基)-2,4-咪唑啉二酮羧酸酯, 生物活性

Based on the 5-(4-hydroxybenzyl)-2,4-imidazolidinedione esters synthesized by simulating the structure of natural inhibitor of AdSS synthetase, twenty eight novel compounds 5-(4-hydroxyphenyl)-2,4- imidazolidinedione esters were synthesized using 5-(4-hydroxyphenyl)-2,4-imidazolidinedione as the key intermediate. Their structures were confirmed by m.p., IR, 1H NMR techniques and elemental analysis. The preliminary bioassay results indicated that 5-(4-hydroxyphenyl)-2,4-imidazolidinedione p-tert-butylbenzoate (2i) and 2-thiophenate (3b) have an inhibitory ratio 70% against Arabidopsis thaliana at the concentration of 200 μg/mL.

Key words: AdSS inhibitor, 5-(4-hydroxyphenyl)-2,4-imidazolidinedione ester, bioactivity