5-芳甲氧基-3(2H)-哒嗪酮衍生物的设计、合成与生物活性有机化学.pdfVIP

2007 年第 27 卷 有 机 化 学 Vol. 27, 2007 第 6 期, 763～767 Chinese Journal of Organic Chemistry No. 6, 763～767 ·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 ( 中国农业大学应用化学系 北京 100094) 摘要 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 哒嗪酮; 合 ; 生物活性; 构效关系 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 (Department of Applied Chemistry , China Agricultural University, Beijing 100094) Abstract In order to search for new insect growth regulators, fifteen new compounds containing 5-oxo- 1 3(2H)-pyridazinone derivatives were designed and synthesized. Their structures were confirmed by H 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 relation- ship of compounds was also discussed. Keywords 3(2H)-pyridazinone; synthesis; biological activity; structure-activity relationship 近年来, 杂环类化合物因其良好的生物活性和结构 性, 同时探索 3(2H)-哒嗪酮环 5 位取代基的变化对生物 可修饰性成为新农药研究开发的热