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Design, synthesis and bioactivity evaluation of novel acylthiourea derivatives of cantharidin

文献类型： 外文期刊

作者： Wang, Mei-Juan 1 ; Nan, Xiang 1 ; Feng, Gang 3 ; Yu, Hai-Tao 2 ; Hu, Guan-Fang 2 ; Liu, Ying-Qian 1 ;

作者机构： 1.Lanzhou Univ, Sch Pharm, Lanzhou 730000, Peoples R China

2.Gansu Acad Agr Sci, Inst Plant Protect, Lanzhou 730070, Peoples R China

3.Chinese Acad Trop Agr Sci, Environm & Plant Protect Inst, Danzhou 571737, Peoples R China

关键词： Cantharidin;Acaricidal activity;Insecticidal activity;Structure-activity relationship

期刊名称：INDUSTRIAL CROPS AND PRODUCTS （ 影响因子：5.645； 五年影响因子：5.749 ）

ISSN： 0926-6690

年卷期： 2014 年 55 卷

页码：

收录情况： SCI

摘要： In an attempt to find the biorational pesticides, a series of novel acylthiourea derivatives of cantharidin were designed, synthesized and preliminarily evaluated for their bioactivities against Tetranychus cinnabarinus and Brevicoryne brassicae. All the new compounds showed significant acaricidal activities against T. cinnabarinus with LC50 values ranging from 0.695 to 2.934 mmol/L. In particular, compounds 6i and 6g exhibited the greatest acaricidal activity against T. cinnabarinus in all derivatives we prepared. Moreover, all of these compounds displayed better acaricidal activities against T. cinnabarinus than insecticidal activities against B. brassicae. Based on the observed bioactivities, the structure-activity relationship (SAR) of these analogs was also discussed. The present work indicated that some cantharidin derivatives can be used as potential lead compounds for developing novel insecticides and acaricides. (C) 2014 Elsevier B.V. All rights reserved.

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