title: Intermediate derivatisation method in the discovery of new acaricide candidates: synthesis of N-substituted piperazine derivatives and their activity against phytophagous mites.
abstract: BACKGROUND
  To discover and exploit novel acaricidal compounds, a series of novel N-substituted piperazine derivatives were designed and synthesised using a tert-butyl piperazine-1-carboxylate as the starting material by intermediate derivatisation methods, and their acaricidal activities were evaluated.
  
  
  RESULTS
  Compounds 11 and 12 exhibited significant acaricidal activity against adults of Tetranychus cinnabarinus in greenhouse tests. Compound 12, in particular, was found to be the best potential candidate acaricide and proved to be more active than the commercial positive controls spirodiclofen and pyridaben, with an LC50of 0.8977 mg L-1. Results concerning acaricidal activity against larvae and eggs of T. cinnabarinus indicated that compound 12 possessed equivalent larvicidal activity to spirodiclofen and higher larvicidal activity than pyridaben. Meanwhile, compound 12 showed less ovicidal activity than pyridaben, but higher activity than spirodiclofen. Furthermore, the results of the field trial demonstrated that compound 12 could effectively control Panonychus citri and P. ulmi with long-lasting persistence and rapid action.
  
  
  CONCLUSIONS
  The present work indicates that compound 12 could be a novel acaricide candidate for spider mite control. © 2016 Society of Chemical Industry.
authors.affiliation: State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Sinochem Agrochemicals R&D Co. Ltd, Shenyang, China.|State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Research Institute of Chemical Industry Co. Ltd, Shenyang, China.
authors.forename: Yong
authors.initials: Y
authors.lastname: Xie
authors.affiliation: State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Research Institute of Chemical Industry Co. Ltd, Shenyang, China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Xu
authors.affiliation: State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Sinochem Agrochemicals R&D Co. Ltd, Shenyang, China.|State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Research Institute of Chemical Industry Co. Ltd, Shenyang, China.
authors.forename: Changling
authors.initials: C
authors.lastname: Liu
authors.affiliation: State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Sinochem Agrochemicals R&D Co. Ltd, Shenyang, China.|State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Research Institute of Chemical Industry Co. Ltd, Shenyang, China.
authors.forename: Aiying
authors.initials: A
authors.lastname: Guan
authors.affiliation: State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Sinochem Agrochemicals R&D Co. Ltd, Shenyang, China.
authors.forename: Lanfeng
authors.initials: L
authors.lastname: Ban
authors.affiliation: College of Agriculture and Plant Protection, Qingdao Agricultural University, Qingdao, China.
authors.forename: Fei
authors.initials: F
authors.lastname: Ding
authors.affiliation: College of Agriculture and Plant Protection, Qingdao Agricultural University, Qingdao, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Peng
mesh_terms: D056810:Acaricides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D001681:Biological Assay; D060326:Chemistry Techniques, Synthetic; D015195:Drug Design; D004780:Environment, Controlled; D007814:Larva / Q000187:drug effects; D008925:Mites / Q000187:drug effects*; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D056810:Acaricides; D010879:Piperazines
keywords: N-substitituted piperazine derivatives; acaricidal activity; intermediate dervatisation method; new acaricide candidate