Synthesis and Biological Evaluation of Novel Anthranilic Diamides Containing N-H/CH3-1H-Pyrazole

• 作 者: ZHANG Xiulan ZHANG Huan LIU Jingbo XIONG Lixia LI Zhengming
• 机 构: College of Science, Tianjin University of Science & Technology, Tianjin 300457, P.R.China;State Key
• 出 处: 高等学校化学研究（英文版）
• 发表日期: 2020年5期
• 关键词: Anthranilic diamide Insecticidal activity Fungicidal activity Antitumor activity

In order to systematically study the structure-activity relationship of anthranilic diamides and develop insecticides with simple structure and high efficiency,a series of novel anthranilic diamides containing N-H/CH3-1H-pyrazole was designed and synthesized.Their chemical structures were characterized by 1H NMR spectra,high resolution mass spectrometry(HRMS) or 13C NMR spectra.The preliminary bioassay results indicated that all title compounds displayed moderate insecticidal activity against oriental armyworm(Mythimna separata) at 200 mg/L and fungicidal activities against six kinds of fungi at 50 mg/L,especially compound 5i showed 50％ insecticidal activity at 25 mg/L.In addition,some compounds exhibited certain antitumor activities.It was demonstrated that the introduction of CH3 group into pyrazole ring was superior to H for the insecticidal activity.