摘要
为发现高抑菌活性的先导化合物,结合本课题组前期研究,设计并合成了17个新型含肟酯的吡唑衍生物,结构经1H NMR、13C NMR及高分辨质谱分析确证,化合物7q的结构经单晶衍射确证。抑菌活性测定结果表明,目标化合物在50μg/mL下对苹果树腐烂病菌Valsa mali、油菜菌核病菌Sclerotinia sclerotiorum、番茄灰霉病菌Botrytis cinerea和小麦全蚀病菌Gaeumannomyces graminis均表现出一定的抑制活性,其中化合物7q对番茄灰霉病菌的抑制活性较好,EC50值为7.04μg/mL,优于先导化合物L1和肟菌酯。
In order to discover lead compound with high antifungal activities,17 novel pyrazole derivatives containing oxime esters were designed and synthesized based on our previous studies.Their structures were characterized by 1H NMR,13C NMR and HRMS,and the crystal structure of compound 7q was confirmed by X-ray diffraction.The bioassay results showed that target compounds displayed antifungal activities against Valsa mali,Sclerotinia sclerotiorum,Botrytis cinerea and Gaeumannomyces graminis.Especially,compound 7q exhibited satisfied activity against B.cinerea with the EC50 value of 7.04μg/mL,which was better than that of the lead compound(L1)and trifloxystrobin.
作者
沈安泽
胡恩畅
刘函如
王宇佳
王勇
马志卿
冯俊涛
雷鹏
SHEN Anze;HU Enchang;LIU Hanru;WANG Yujia;WANG Yong;MA Zhiqing;FENG Juntao;LEI Peng(College of Plant Protection,Northwest A&F University,Yangling 712100,Shaanxi Province,China)
出处
《农药学学报》
CAS
CSCD
北大核心
2021年第1期69-75,共7页
Chinese Journal of Pesticide Science
基金
西北农林科技大学科研启动费(00200-Z109021809)
省级大学生创新创业训练计划项目(S201910712256).
关键词
肟酯
吡唑衍生物
合成
抑菌活性
oxime ester
pyrazole
synthesis
antifungal activity
