新型含嘧啶环结构的吡唑肟类衍生物的合成及其生物活性研究
收稿日期: 2016-11-30
修回日期: 2017-01-04
网络出版日期: 2017-01-17
基金资助
国家自然科学基金（No.21372135）、江苏省“六大人才高峰”（No.2013-SWYY-013）和南通大学研究生科研创新计划（No.YKC16086）资助项目.
Synthesis and Biological Activities of Novel Pyrazole Oximes Containing Substituted Pyrimidine Group
Received date: 2016-11-30
Revised date: 2017-01-04
Online published: 2017-01-17
Supported by
Project supported by the National Natural Science Foundation of China (No. 21372135), the Research Foundation of the Six People Peak of Jiangsu Province (No. 2013-SWYY-013), and the Science and Technology Innovation Foundation for the Graduate Students of Nantong University (No. YKC16086).
为了从吡唑肟类化合物中寻找新的活性物质，通过活性亚结构拼接方法，设计并合成了一系列未见文献报道的新型含取代嘧啶环结构的吡唑肟类衍生物. 采用1H NMR，13C NMR，MS和元素分析确认了目标化合物的结构. 初步的生物活性测试结果表明，部分化合物显示出一定的杀虫活性. 在测试浓度为500 μg/mL时，化合物6b和6c对蚜虫的杀死率分别为60%和70%，化合物6a，6b，6c和6d对褐飞虱的杀灭效果分别为100%，100%，100%和90%. 当测试浓度降至100 μg/mL时，化合物6a，6b和6d对褐飞虱仍表现出中等水平的杀虫效果，其杀死率分别为60%，60%和50%. 此外，化合物6f，6g和6m在测试浓度为500 μg/mL时对粘虫的杀死率分别为80%，70%和90%.
戴红 , 叶林玉 , 李阳 , 方源 , 石玉军 , 梁志鹏 , 石健 . 新型含嘧啶环结构的吡唑肟类衍生物的合成及其生物活性研究[J]. 有机化学, 2017 , 37(4) : 1020 -1026 . DOI: 10.6023/cjoc201611042
In order to explore novel potent pesticide from pyrazole oxime derivatives, a series of new pyrazole oxime compounds carrying substituted pyrimidine moiety were synthesized by the method of active substructure combination. The structures of the title compounds were characterized by 1H NMR, 13C NMR, MS and elemental analysis. Preliminary bioassay data displayed that some target compounds showed certain insecticidal activities. At the concentration of 500 μg/mL, compounds 6b and 6c exhibited 60% and 70% insecticidal activity against Aphis craccivora, compounds 6a, 6b, 6c, and 6d had 100%, 100%, 100% and 90% insecticidal activity against Nilaparvata lugens. When the concentration was reduced to 100 μg/mL, compounds 6a, 6b and 6d were still active against Nilaparvata lugens with inhibitory values of 60%, 60% and 50%, respectively. In addition, insecticidal activities against Oriental armyworm of compounds 6f, 6g and 6m were 80%, 70% and 90%, respectively, at 500 μg/mL.
Key words： pyrimidine; pyrazole oxime; synthesis; bioactivity
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