高等学校化学学报

高等学校化学学报

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2-甲基-1-(4-芳基噻唑-2-基)-苯并咪唑-6-甲酸乙酯的合成、表征及生物活性

胡艾希1, 贺丽敏1, 董敏宇1, 张建宇1,2, 欧晓明2   

    1. 湖南大学化学化工学院, 长沙 410082;
    2. 国家农药创制工程技术研究中心, 长沙 410007
  • 收稿日期:2007-09-19 修回日期:1900-01-01 出版日期:2008-04-10 发布日期:2008-04-10
  • 通讯作者: 胡艾希

Synthesis, Characterization and Biological Activity of Ethyl 2-Methyl-1-(4-arylthiazol-2-yl)-benzoimidazole-6-carboxylate

HU Ai-Xi1*, HE Li-Min1, DONG Min-Yu1, ZHANG Jian-Yu1,2, OU Xiao-Ming2   

    1. College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China;
    2. National Engineering Research Center for Agrochemicals, Changsha 410007, China
  • Received:2007-09-19 Revised:1900-01-01 Online:2008-04-10 Published:2008-04-10
  • Contact: HU Ai-Xi

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被引次数

25

摘要： 以4-乙酰氨基苯甲酸乙酯为原料设计合成了14 种2-甲基-1-(4-芳基噻唑-2-基)-苯并咪唑-6-甲酸乙酯新化合物. 化合物结构经质谱、1H NMR、红外光谱和元素分析等确证, 并用单晶X射线衍射仪测定了化合物5a的晶体结构. 生物活性实验结果表明, 化合物5c(500 mg/L)对小麦白粉病菌抑制率达到95%; 化合物5e对辣椒疫霉病菌(25 mg/L)的抑制率为61.9%, 对油菜菌核病菌(500 mg/L) 抑制率高达97.2%; 化合物5k(25 mg/L) 对小麦赤霉病菌抑制率为55.1%.

关键词: 2-甲基-1-(4-芳基噻唑-2-基)-苯并咪唑-6-甲酸乙酯, 生物活性, 晶体结构

Abstract: Compounds containing thiazole or benzoimidazole ring system are found to exhibit a wide spectrum of biological activities. Fourteen new ethyl 2-methyl-1-(4-arylthiazol-2-yl)-benzoimidazole-6-carboxylates were synthesized from ethyl 4-acetamidobenzoate with four steps. Their structures were clearly established by MS, 1H NMR spectra and elemental analysis. The crystal structure of compound 5a was determined by X-ray diffraction analysis. The preliminary bioassays indicate that compound 5c exhibited 95% inhibition rate against E. graminis at 500 mg/L; compound 5e exhibited 61.9% inhibition rate against P. capsici at 25 mg/L. compound 5e exhibited 97.2% inhibition rate against S. sclerotiorum at 500 mg/L, and compound 5k exhibited 55.1% inhibition rate against G. zeae.

Key words: Ethyl 2-methyl-1-(4-arylthiazol-2-yl)-benzoimidazole-6-carboxylate, Biological activity, Crystal structure

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