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苯基吡唑氧基丙酸衍生物的设计、合成及其对水稻纹枯病的杀菌活性(英文)
引用本文:于福强,关爱莹,孙旭峰,李慧超,李小武.苯基吡唑氧基丙酸衍生物的设计、合成及其对水稻纹枯病的杀菌活性(英文)[J].有机化学,2019(2):397-405.
作者姓名:于福强  关爱莹  孙旭峰  李慧超  李小武
作者单位:东北大学材料科学与工程学院材料物理与化学系材料各向异性与织构教育部重点实验室;沈阳中化农药化工研发有限公司新农药创制与开发国家重点实验室
基金项目:Project supported by the Liaoning Provincal Science and Technology Plan Projects(No.2015306001)~~
摘    要:水稻纹枯病是水稻的三大病害之一,发病后可造成水稻严重减产,使用杀菌剂是使水稻免遭病害侵扰的有效途径之一.由于杀菌剂使用一段时间后病菌不可避免地会对其产生抗药性,因此需要不断开发结构新颖的化合物.采用中间体衍生化方法,设计并合成了25个结构新颖的苯基吡唑氧基丙酸衍生物.所有化合物都进行了离体生物活性测试,并讨论了构效关系.生物活性测试数据表明,结构新颖的苯基吡唑氧基丙酸衍生物对水稻纹枯病菌均具有良好的抑制作用,其中2-((1-(4-氯苯基)-1H-吡唑-3-基)氧基)-N-(4-硝基苯基)丙酰胺(17)(EC50=1.05 mg/L)和2-((1-(4-氯苯基)-1H-吡唑-3-基)氧基)-N-(吡啶-2-基)丙酰胺(22)(EC50=1.02 mg/L)对水稻纹枯病菌的杀菌活性与对照药物戊唑醇(EC50=1.02 mg/L)相当;2-((1-(4-氯苯基)-1H-吡唑-3-基)氧基)-N-(3,4-二氯苯基)丙酰胺(20)(EC50=0.95 mg/L)活性略优于商品化对照药剂戊唑醇(EC50=1.02 mg/L).

关 键 词:苯基吡唑氧基丙酸衍生物  中间体衍生化  杀菌活性  水稻纹枯病  构效关系

Design,Synthesis and Fungicidal Activity against Rhizoctonia solani of New Phenylpyrazoloxyl Propionic Acid Derivatives
Yu Fuqiang,Guan Aiying,Sun Xufeng,Li Huichao,Li Xiaowu.Design,Synthesis and Fungicidal Activity against Rhizoctonia solani of New Phenylpyrazoloxyl Propionic Acid Derivatives[J].Chinese Journal of Organic Chemistry,2019(2):397-405.
Authors:Yu Fuqiang  Guan Aiying  Sun Xufeng  Li Huichao  Li Xiaowu
Affiliation:(Key Laboratory for Anisotropy and Texture of Materials, Ministry of Education, Department of Materials Physics and Chemistry, School of Material Science and Engineering, Northeastern University, Shenyang 110819;State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Sinochem Agrochemicals R & D. Co. Ltd., Tiexi District, Shenyang 110021)
Abstract:Yu Fuqiang;Guan Aiying;Sun Xufeng;Li Huichao;Li Xiaowu(Key Laboratory for Anisotropy and Texture of Materials, Ministry of Education, Department of Materials Physics and Chemistry, School of Material Science and Engineering, Northeastern University, Shenyang 110819;State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Sinochem Agrochemicals R & D. Co. Ltd., Tiexi District, Shenyang 110021)
Keywords:phenylpyrazoloxyl propionic acid derivatives  intermediate derivatization method  fungicidal activity  Rhizoctonia solani  strueture-activity relationship
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