新型2-甲基-3-呋喃甲酰胺类化合物的设计、合成及抑菌活性研究  

Design,synthesis and antifungal activity of novel 2-methyl-3-furancarboxamide derivatives

作　　者：蒲桃 王宏宇[1] 刘英[1] 金洪[1] 陶科[1] 侯太平[1] 

机构地区：[1]四川大学生命科学学院生物资源与生态环境教育部重点实验室,成都610064

出　　处：《四川大学学报（自然科学版）》2017年第1期178-184,共7页Journal of Sichuan University(Natural Science Edition)

基　　金：国家自然科学基金(31272068)

摘　　要：为寻找高活性抑菌化合物,20种以杀菌剂甲呋酰胺为结构基础的新型2-甲基-3-呋喃甲酰胺类化合物经过设计并合成,它们的结构已通过氢核磁确定.接着,选取5种常见且具有代表性的植物病原真菌(水稻纹枯病菌、油菜菌核病菌、马铃薯晚疫病菌、番茄绵腐病菌、苹果轮纹病菌)作为供试菌种,采用生长速率法对所合成的目标化合物进行了抑菌活性初步筛选.结果表明:在浓度为20mg/L时,化合物1e,1f,2a,2b和2f对水稻纹枯病菌的校正抑菌率分别为88.6%、74.5%、78.5%、78.7%和73.1%,优于阳性对照甲呋酰胺(70.5%).进一步对5种化合物抑制水稻纹枯病菌有效中浓度(EC_(50))的测定,发现化合物1e的EC_(50)值为2.824mg/L,优于阳性对照杀菌剂甲呋酰胺(EC_(50)=7.691mg/L).表明化合物1e对水稻纹枯病菌抑菌活性最强,可作为先导化合物进一步结构优化.Based on the structure of the fungicide fenfuram for exploring high antifungal agents, twenty novel 2-methyl-3-furancarboxamide derivatives were designed, synthesized and characterized by1 H NMR. Then, their in vitro antifungal activities were evaluated against five normal phytopathogenic fungi （Rhizoctonia solani , Sclerotinia sclerotiorurn , Ph ytophthora in f estans , P ythium a phanidermatum and Physalospora piricola） by mycelial growth inhibition method. In conclusion, compounds le, 1f, 2a, 2b and 2f exhibited stronger antifungal effects on R. solani with inhibition rates of 88. 6 %, 74.5 %, 78.5 %, 78.7% and 73.1%, respectively, superior to commercial fungicide fenfuram （70.5%）. The ECho values of the five tested compounds against R. solani showed that compound le exhibited the most potent inhibition with an EC50 value of 2. 824 mg/L which lower than that of fenfuram （EC50 = 7. 691 mg/L）. As a result, compound le could be a lead compound for further research.

关 键 词：2-甲基-3-呋喃甲酰胺类 合成 抑菌活性 EC50 

分 类 号：S482.2[农业科学—农药学]