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有机化学
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有机化学 ›› 2011, Vol. 31 ›› Issue (10): 1648-1652. 上一篇    下一篇

研究论文

N-[3-(4-喹唑啉基)氨基-1H-吡唑-4-甲酰基]醛腙类衍生物的合成及抗菌活性研究

高元磊，林选福，韩菲菲，鲍小平*   

  1. (贵州大学精细化工研究开发中心 教育部绿色农药与农业生物工程重点实验室 贵阳 550025)
  • 收稿日期:2011-04-06 修回日期:2011-05-13 发布日期:2011-06-10
  • 通讯作者: 鲍小平 E-mail:baoxp_1980@yahoo.com.cn

Synthesis and Fungicidal Activities of N-[(3-(4-Quinazolinyl)- amino-1H-pyrazole-4-formyl)aldehyde Hydrazones

GAO Yuan-Lei, LIN Xuan-Fu, HAN Fei-Fei, BAO Xiao-Ping   

  1. (Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025)
  • Received:2011-04-06 Revised:2011-05-13 Published:2011-06-10

PDF

1504

被引次数

37

以4-氯喹唑啉、3-氨基-4-吡唑甲酸乙酯和芳醛为原料, 合成了13个新型的N-[3-(4-喹唑啉基)氨基-1H-吡唑-4-甲酰基]醛腙类化合物, 通过IR, 1H NMR, 13C NMR和元素分析对其结构进行了确认. 初步生物活性测试结果表明, 在50 μg/mL浓度下, 化合物5d对小麦赤霉菌和苹果腐烂菌的抑制率与对照药剂噁霉灵相当|化合物5k对小麦赤霉菌的抑制率则高于噁霉灵.

关键词: 喹唑啉, 吡唑, 酰腙, 合成, 抗菌活性

Using 4-chloroquinazoline, ethyl 3-amino-4-pyrazolecarboxylate and aromatic aldehyde as starting compounds, thirteen novel N-[(3-(4-quinazolinyl)amino-1H-pyrazole-4-formyl]aldehyde hydrazones were synthesized. Their structures were confirmed by IR, 1H NMR, 13C NMR spectra and elemental analysis. Preliminary bioassay indicated that compound 5d exhibited similar antifungal activities against Gibberella zeae and Cytospora mand-shurica at 50 μg/mL, compared with control agent (hymexazol). In addition, compound 5k possessed higher inhibition rate against G. zeae than hymexazol.

Key words: quinazoline, pyrazole, acyl hydrazone, synthesis, fungicidal activity