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有机化学
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有机化学 ›› 2007, Vol. 27 ›› Issue (06): 763-767. 上一篇    下一篇

研究论文

5-芳甲氧基-3(2H)-哒嗪酮衍生物的设计、合成与生物活性

凌云，李洪森，杨新玲*，鲍涵，邱立红，陈馥衡   

  1. (中国农业大学应用化学系 北京 100094)
  • 收稿日期:2006-02-20 修回日期:2007-08-31 发布日期:2007-05-21
  • 通讯作者: 杨新玲

Design, Synthesis and Biological Activity of 5-Oxo-3(2H)-pyridazinone Derivatives

LING Yun, LI Hong-Sen, YANG Xin-Ling*, BAO Han
QIU Li-Hong, CHEN Fu-Heng   

  1. (Department of Applied Chemistry, China Agricultural University, Beijing 100094)
  • Received:2006-02-20 Revised:2007-08-31 Published:2007-05-21
  • Contact: YANG Xin-Ling

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为寻找新型昆虫生长调节活性化合物, 设计合成了15个未见文献报道的5-芳甲氧基取代的3(2H)-哒嗪酮衍生物, 所有化合物结构均通过1H NMR, IR和元素分析确证. 初步生物活性研究表明, 化合物8o对2龄家蝇幼虫有明显的抑制作用; 化合物8a, 8c, 8g和8j对3龄蝗蝻显示出较好的生物活性. 对目标化合物的构效关系亦进行了初步探讨.

关键词: 合成, 生物活性, 构效关系, 哒嗪酮

In order to search for new insect growth regulators, fifteen new compounds containing 5-oxo- 3(2H)-pyridazinone derivatives were designed and synthesized. Their structures were confirmed by 1H NMR, IR Spectra and elemental analysis. In the preliminary bioassay test, compound 8o obviously disrupted the development of second-instar housefly larvae. Compounds 8a, 8c, 8g and 8j also showed good activity against the third-instar nymphs of locusts (Locusta migratoria manilensis). The structure-activity relationship of compounds was also discussed.

Key words: synthesis, biological activity, structure-activity relationship, 3(2H)-pyridazinone