为了从吡唑类化合物中寻找具有新的活性物质,利用亚结构拼接原理,设计合成了一系列新型含取代异噁唑结构的吡唑酰胺类衍生物.利用1H NMR、13C NMR和元素分析对标题化合物的结构进行了表征.初步的生物活性测试结果表明,部分目标化合物具有较好的杀虫活性.在测试浓度为500μg/m L时,部分化合物对粘虫的防效为60%~100%,对蚜虫的杀死率分别为50%~100%.另外,部分化合物对Hep G2细胞显示出较好的抗肿瘤活性,其IC50值为14.2~18.9μmol/L.
In order to find novel pyrazole compounds possessing potent biological activities, a series of novel pyrazole amide derivatives bearing substituted isoxazole moiety were designed and synthesized according to the method of active substructure combination. Their structures were confirmed by 1H NMR, 13 C NMR and elemental analysis. The bioassay data indicated that some title compounds had good insecticidal activities. At the concentration of 500 μg/m L, some compounds showed 60%~100% insecticidal activity against Oriental armyworm, and 50%~100% insecticidal activity against Aphis medicaginis. Additionally, some compounds exhibited good anti-cancer activity against Hep G2 cells with the IC50 values of 14.2~18.9 μmol/L.