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Novel Trifluoromethylpyrazole Acyl(Thio)Urea Derivatives:Synthesis,Crystal Structure, Fungicidal Activity and Docking Study

Tao Jin  Zhi-Wen Zhai  Zhong-Hua Shen  Ya-Xin Zhao  Yan-Xia Shi  Cheng-Xia Tan  Jian-Quan Weng  Bao-Ju Li  Xing-Hai Liu  
【摘要】:Twenty three novel trifluoromethylpyrazole acyl urea and acyl thiourea derivatives were designed and synthesized.In vivo fungicidal activities of these compounds were tested against Fusarium oxysporum,Corynespora mazei,Botrytis cinerea and Pseudomonas syringae respectively,particularly compounds exhibited significant control effective at 100 mg/L.More importantly,some compounds showed the good control effective at 10 mg/L.Furthermore,docking was established to study the structure-activity relationship of the title compounds.It is possible that trifluoromethylpyrazole acyl urea and acyl thiurea derivatives,which possess good control effective against Fusarium oxysporum,Corynespora mazei and Botrytis cinerea,may become novel lead compounds for the development of fungicides with further structure modification.

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