5-取代苯甲酰基脲-3(2H)-哒嗪酮衍生物的合成及昆虫生长调节活性

Synthesis and Insect Growth Regulating Activity of 5-Benzoylphenylurea-3(2H)-Pyridazinone

哒嗪酮是一类具有良好生物活性的杂环,为进一步发现具有昆虫生长调节活性的新型化合物,依据前期研究成果,在3(2H)-哒嗪酮的5位上引入苯甲酰基脲活性基团,设计合成了17个5-取代苯甲酰基脲-3(2H)-哒嗪酮衍生物,并通过两种方法制备得到了目标化合物,结构均通过1HNMR、IR和元素分析确证。初步生物活性研究结果表明,部分化合物如6a、BPU-4在200mg/L时对3龄蝗蝻Locusta migratoria manilensisLinne(Meyen)有较好的生物活性,使蝗蝻因不能正常蜕皮变态而死亡,表现出明显的昆虫生长调节剂(IGRs)类化合物的作用特征。

Pyridazinone is a family of heterocycle with good biological activity.In order to find new insect growth regulators,benzoylphenylurea was introduced into 5-position of 3（2H）-pyridazinone ring based on the former research.Seventeen 5-benzoylphenylurea-3（2H）-pyridazinones were designed by linking sub-active group and synthesized in two methods.Their structures were confirmed by ^1H NMR,IR and elemental analysis.In the preliminary bioassay test,some compounds such as 6a,BPU-4 showed good activity against the third-instar nymphs of locusts（Locusta migratoria manilensis Linne）（Meyen）at the concentration of 200mg/L.The title compounds,disrupting the growth and development of treated nymphs of locusts,exhibited obviously the effect as insect growth regulator（IGRs）.