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Design, synthesis and bioactivity evaluation of novel benzophenone hydrazone derivatives

文献类型： 外文期刊

作者： Li, Wen-Qun 1 ; Zhang, Zhi-Jun 1 ; Nan, Xiang 1 ; Liu, Ying-Qian 1 ; Hu, Guan-Fang 2 ; Yu, Hai-Tao 2 ; Zhao, Xiao-Bo 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

关键词： benzophenone hydrozone;thiourea;urea;acaricide;insecticide;structure-activity relationship

期刊名称：PEST MANAGEMENT SCIENCE （ 影响因子：4.845； 五年影响因子：4.674 ）

ISSN：

年卷期：

页码：

收录情况： SCI

摘要： BACKGROUND: Benzophenone hydrazone derivatives are among the most important classes of synthetic insecticides. In an effort to discover new molecules with good insecticidal/acaricidal activities, a series of novel benzophenone hydrazone W-acylated thiourea and urea derivatives was synthesized and bioassayed. RESULTS: All of these compounds exhibited excellent bioactivities against T. cinnabarinus and B. brassicae, especially towards T. cinnabarinus with LC_(50) values ranging from 0.305 to 2.036 mmol L~(-1). Moreover, the acaricidal activities against T. cinnabarinus of compounds 8a-i, 12b-f and 12h were 2.5-5.5-fold that of parent molecule 3 based on the LC_(50) value. CONCLUSION: Based on the observed bioactivities, the structure-activity relationship of these analogs was also discussed. Structure-activity relationships provided information that could direct further investigation on structure modification. Our studies indicated that benzophenone hydrazone W-acylated thiourea and urea derivatives could be used as potential lead compounds for developing novel acaricides and insecticides.

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