Phytophagous mites, such as Tetranychus cinnabarinus, Panonychus citri and Panonychus ulmi are most important and highly polyphagous pests of a wide range of field and greenhouse crops worldwide. They attack glasshouse as well as field crops causing serious damage by direct feeding or by transmitting plant pathogens and viruses. At present, spider mites such as Tetranychus urticae have developed resistance to virtually all chemical classes to control them. Thus, discovering and exploiting acaricidal compounds with new modes of action becomes an important way to overcome resistance problems.Hence, a series of novel N-substituted piperazines derivatives were designed and synthesized by intermediate derivatization methods and their acaricidal activities were evaluated. The acaricidal activity in greenhouse tests showed some compounds exhibited significant acaricidal activity in controlling adults of Tetranychus cinnabarinus. Compound 623 in particular was found to be the best potential candidate acaricide and proved more active than the contrast spirodiclofen and pyridaben. The results of acaricidal activities against larvae and eggs of Tetranychus cinnabarinus indicated that compound 623 possessed equivalent larvicidal activity to spirodiclofen. Meanwhile, compound 623 showed more ovicidal activity than spirodiclofen. Then, the structure-activity relationships (SARs) of was studied. The present work indicates that compound 623 may be a novel acaricide candidate for spider mites control.

Design, synthesis, and the structure-activity relationships of novel N-substituted piperazines derivatives

252nd National Meeting (2016)

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