Novel quinoxalinone-1,2,3-triazole derivatives as potential antifungal agents for plant anthrax disease:Design,synthesis,antifungal activity and SAR study  

作　　者：Yu Jiang Chang-Heng Zhu Zi-Hao Xia Han-Qing Zhao 

机构地区：[1]Key Laboratory for Northern Urban Agriculture of Ministry of Agriculture and Rural Affairs,Beijing University of Agriculture,No.7 Beinong Road,102206,Changping District,Beijing,China

出　　处：《Advanced Agrochem》2024年第3期222-228,共7页现代农业化学（英文）

基　　金：financial support by the Natural Science Foundation of Beijing(No.2232004);Research Fund for Academic Degree&Graduate Education of Beijing University of Agriculture(2023YJS021);Science and Technology innovation support program of Beijing University of Agriculture(BUA-HHXD2023008);R&D Program of Beijing Municipal Education Commission(No.KM202210020007);Research and Innovation Ability Improvement Project for Young Teachers of Beijing University of Agriculture(QJKC2022014).

摘　　要：A series of quinoxalinone-1,2,3-triazole derivatives have been synthesized and tested for antifungal activity against phytopathogenic fungus through mycelial growth inhibition in vitro,spore germination inhibition in vitro and control effect in vivo.The results showed that the pharmacophore quinoxalinone and 1,2,3-triazole displayed promising antifungal activity.The EC50 value against C.gloeosporioides of 6a-1 was 1.17μg/mL and the compound 6c-1 showed the good bioactivity against C.fragariae Brooks and P.oryzae Cav.,displaying EC50 values of 5.56,4.62μg/mL,respectively.The inhibitory of spore germination by 6a-1 was performed with EC50 value of 1.91μg/mL.In addition,the in vivo bioassay indicated that 6a-1 possessed effective control against Pepper Anthrax Disease in protective treatment.For given activity data of target compounds,structure-activity relationship(SAR)study was operated,hoping for optimizing the target structure to find lead compound with higher activity.

关 键 词：Molecules design PESTICIDES Antifungal activity SAR study 

分 类 号：O62[理学—有机化学]