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论文摘要

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(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);王宏宇(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);刘英(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);金洪(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);陶科(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);侯太平(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)

Author:PU Tao(Key Laboratory of Bio-resources and Eco-environment of Ministry of Education, College of Life Sciences, Sichuan University);WANG Hong-Yu(Key Laboratory of Bio-resources and Eco-environment of Ministry of Education, College of Life Sciences, Sichuan University);LIU Ying(Key Laboratory of Bio-resources and Eco-environment of Ministry of Education, College of Life Sciences, Sichuan University);JIN Hong(Key Laboratory of Bio-resources and Eco-environment of Ministry of Education, College of Life Sciences, Sichuan University);TAO Ke(Key Laboratory of Bio-resources and Eco-environment of Ministry of Education, College of Life Sciences, Sichuan University);HOU Tai-Ping(Key Laboratory of Bio-resources and Eco-environment of Ministry of Education, College of Life Sciences, Sichuan University)

收稿日期:2015-05-18          年卷(期)页码:2017,54(1):178-184

期刊名称:四川大学学报: 自然科学版

Journal Name:Journal of Sichuan University (Natural Science Edition)

关键字:2-甲基-3呋喃甲酰胺类;合成; 抑菌活性; EC50

Key words:2-methyl-3-furancarboxamide derivatives; Synthesis; Antifungal activity; EC50

基金项目:国家自然科学基金

中文摘要

摘要:20种以杀菌剂甲呋酰胺为结构基础的新型2-甲基-3呋喃甲酰胺类系列化合物经过设计并合成得到,它们的结构通过氢核磁确定. 采用生长速率法,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对所合成的目标化合物进行了抑菌活性初步筛选.在浓度为20 mg/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 %). 通过进一步对5种化合物对水稻纹枯病菌的抑制有效中浓度(EC50)测定,发现化合物1e的EC50值最低,为2.824 mg/L,优于阳性对照杀菌剂甲呋酰胺(EC50 = 7.691 mg/L).表明化合物1e对水稻纹枯病句显示出较强抑菌活性,可作为先导化合物进一步结构优化.

英文摘要

Abstract: Based on the structure of the fungicide fenfuram, twenty novel 2-methyl-3-furancarboxamide derivatives were designed, synthesized characterized by 1H NMR. Their in vitro antifungal activities were evaluated against five normal phytopathogenic fungi Rhizoctonia solani, Sclerotinia sclerotiorum, Phytophthora infestans, Pythium aphanidermatum, Physalospora piricola by mycelial growth inhibition method. Compounds 1e, 1f, 2a, 2b and 2f exhibited stronger antifungal effect on R. solani with inhibition of 88.6 %, 74.5 %, 78.5 %, 78.7 % and 73.1 %, respectively, superior to commercial fungicides fenfuram (70.5 %). The EC50 values of the five tested compounds against R. solani showed that compound 1e exhibited the most potent inhibition with an EC50 value of 2.824 mg/L which lower than fenfuram (EC50 = 7.691 mg/L). As a result, compound 1e could be the lead compound for the following research.

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