新型含取代吡啶结构的吡唑酰胺类化合物的合成与生物活性研究

Synthesis and Biological Activities of Novel Pyrazole Amide Derivatives Containing Substituted Pyridyl Group

为了从吡唑酰胺类化合物中寻找新的活性物质,采用活性基团拼接原理,设计并合成了一系列未见文献报道的新型含取代吡啶结构的吡唑酰胺类衍生物.初步的生物活性测定结果显示,部分目标化合物表现出较好的杀虫活性.在测试浓度为500μg/m L时,10个化合物对粘虫的杀死率可达60%~100%,1个化合物对蚜虫的杀死率为100%.当测试浓度降至100μg/m L时,2个化合物对粘虫的杀死率可达70%~100%,高于对照药唑虫酰胺的防效.此外,当测试浓度降至20μg/m L时,1个化合物对粘虫的杀死率为50%.

In order to find novel pyrazole amides having potent bioactivities, a series of novel pyrazole amide compounds carrying substituted pyridyl moiety were designed and synthesized according to the method of active substructure combination.The preliminary bioassay data showed that some title compounds displayed good insecticidal activities. At the concentration of 500 μg/m L, ten compounds exhibited insecticidal activity against Oriental armyworm with 60%～100%, and one compound indicated insecticidal activity against Aphis medicaginis with 100%. When the concentration was reduced to 100 μg/m L, two compounds still showed insecticidal activity against Oriental armyworm with 70%～100%, which were better than that of the control tolfenpyrad. Additionally, one compound displayed 50% insecticidal activity against Oriental armyworm at the concentration of 20 μg/mL.