6-(哌嗪-1-基)-去氢骆驼蓬碱酰胺衍生物的合成及抑菌活性  

Synthesis and antifungal activity of 6-(piperazin-1-yl)-harmine amide derivatives

作　　者：金秋彤 韩广田 胡冬燕 杨顺义 JIN Qiutong;HAN Guangtian;HU Dongyan;YANG Shunyi(College of Plant Protection,Gansu Agricultural University,Biocontrol Engineering Laboratory of Crop Diseases and Pests of Gansu Province,Lanzhou 730070,China;Department of Pharmacy,Leshan Vocational and Technical College of Sichuan Province,Leshan 614000,Sichuan Province,China)

机构地区：[1]甘肃农业大学植物保护学院,甘肃省农作物病虫害生物防治工程实验室,甘肃兰州730070 [2]乐山职业技术学院药学系,四川乐山614000

出　　处：《农药学学报》2023年第3期595-601,共7页Chinese Journal of Pesticide Science

基　　金：甘肃农业大学自列项目。

摘　　要：为探索6-(哌嗪-1-基)-去氢骆驼蓬碱酰胺衍生物的抑菌活性,结合前期的衍生化研究,设计并合成了15个新型6-(哌嗪-1-基)-去氢骆驼蓬碱衍生物,并对其抑菌活性及构效关系进行了研究。离体抑菌活性测定结果表明,目标化合物在50μg/mL下对番茄灰霉病菌Botrytis cinerea、小麦赤霉病菌Fusarium graminearum、梨树腐烂病菌Valsa pyri、棉花枯萎病菌Fusarium oxysporum均有一定的抑制活性,尤其化合物5j对棉花枯萎病菌表现出较好的活性,抑制率达61.7%,强于阳性对照啶酰菌胺。In order to explore the antifungal activity of 6-(piperazin-1-yl)-harmine amide derivative,based on previous derivative studies,15 novel 6-(piperazin-1-yl)-harmine derivatives were designed and synthesized.The antifungal activity was evaluated and the structure-activity relationship was analyzed.The in vitro bioassay results demonstrated that the target compounds showed antifungal activities against Botrytis cinerea,Fusarium graminearum,Valsa pyri and Fusarium oxysporum,especially compound 5j displayed excellent activity against F.oxysporum with inhibition rate of 61.7%at 50μg/mL,which was better than the positive control boscalid.

关 键 词：去氢骆驼蓬碱 衍生化 抑菌活性 棉花枯萎病菌 

分 类 号：TQ450.1[化学工程—农药化工]