Synthesis,Antimicrobial Activity,and Molecular Docking of Benzoic Hydrazide or Amide Derivatives Containing a 1,2,3-Triazole Group as Potential SDH Inhibitors

• 作者: Yue Ding Ling Zhang Song Yang Zhong Li Pei-Yi Wang
• 来源期刊: 中国化学（英文版）
• 年，卷（期）: 2021,（5）
• 所属期刊栏目: Comprehensive Reports
• 页码范围: 1319-1330
• 页数: 12页
• 语种: 英文
• DOI: 10.1002/cjoc.202100007

摘要

Main observation and conclusion The present study was carried out in an attempt to synthesize a new class of antimicrobial agents containing a 1,2,3-triazole motif formed by classical copper catalyzed click chemistry.Antifungal bioassay results showed that five compounds 5a,5e,5h,5j,and 5k possessed a remarkable growth inhibitory activity against Botryosphaeria dothidea,Rhizoctonia solani and Gibberella zeae with EC50 values within 10.0-0.306 μg/mL The in vitro efficacy was better than those of the commercial agrochemicals Azoxystrobin,Boscalid,and Fluxapyroxad.In vivo trials showed that compound 51 was effective for the control of rice sheath blight and wheat scab with the effects of 75％ and 95％,respectively.Antifungal mechanism studies suggested that target compounds were potential succinate dehy-drogenase inhibitors (SDHIs),which were proposed by the agreeable molecular docking study and restrained SDH activity (IC50 =3.95μg/mL,51).Interestingly,compounds 5r and 5s displayed good antibacterial activity against phytopathogens.In vivo screening of 5r and 5s against rice bacterial blight afforded a superior control effect (up to 51％) than those of commercial agents Bismerthiazol and Thiodiazole copper.The current studies could support some title compounds to be the lead compounds for exploring highly bioactive antimicrobial substrates,particularly the potential SDHIs.