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一些含1,3,4-恶二唑部分的新型白鲜碱基硫醚的半合成及其杀虫活性

Semisynthesis and insecticidal activity of some novel fraxinellone-based thioethers containing 1,3,4-oxadiazole moiety.

作者信息

Guo Yong, Wang Xiaoguang, Fan Jiangping, Zhang Qian, Wang Yi, Zhao Yi, Huang Mengxing, Ding Ming, Zhang Yanbing

机构信息

Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, 450001, Henan Province, People's Republic of China.

College of Agriculture, Shanxi Agriculture University, Taigu 030801, Shanxi Province, People's Republic of China.

出版信息

R Soc Open Sci. 2017 Dec 13;4(12):171053. doi: 10.1098/rsos.171053. eCollection 2017 Dec.

Abstract

Two series of novel fraxinellone-based thioethers containing 1,3,4-oxadiazole moiety were prepared as insecticidal agents against the oriental armyworm, Walker. The structural assignment was based on the spectroscopic and X-ray analysis data. Among all the target compounds, compounds , , , and exhibited more potent insecticidal activity with final mortality rates (FMRs) of more than 65%, especially with the FMR of 75.9%, when compared with toosendanin. Some interesting results of structure-activity relationships are also discussed.

摘要

制备了两个系列含1,3,4-恶二唑部分的新型白鲜碱基硫醚作为防治东方粘虫(Walker)的杀虫剂。结构归属基于光谱和X射线分析数据。在所有目标化合物中,化合物、、、和表现出更强的杀虫活性,最终死亡率(FMRs)超过65%,尤其是与川楝素相比,其FMR为75.9%。还讨论了一些有趣的构效关系结果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/373a/5750010/5cb16952d3be/rsos171053-g1.jpg

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