Design and Synthesis of Novel 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides-based Strobilurins as Potent Fungicide Candidates

作     者：LI Fengyun GONG Jianing LIU Jingbo LI Yuxin LI Zhengming LI Fengyun;GONG Jianing;LIU Jingbo;LI Yuxin;LI Zhengming

作者机构：School of Chinese Materia MedicaTianjin State Key Laboratory of Modern Chinese MedicineTianjin University of Traditional Chinese MedicineTianjin 300193P.R.China College of Horticulture and Landscape ArchitectureTianjin Agricultural UniversityTianjin 300384P.R.China State Key Laboratory of Elemento-Organic ChemistryResearch Institute of Elemento-Organic ChemistryCollege of ChemistryNankai UniversityTianjin 300071P.R.China 

基　　金：Supported by the Scientific Project of Tianin Municipal Education Commission China(No.2018KJ008) 

出 版 物：《Chemical Research in Chinese Universities》 (高等学校化学研究（英文版）)

年 卷 期：2020年第36卷第6期

页      码：1190-1195页

摘      要：To discover novel strobilurins analogues with good and broad spectrum activity,a series of nove 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides-based strobilurins was designed,synthesized,and tested agains various phytopathogenic *** *** 7k exhibited substantial and broad spectrum antifungal activities against the tested phytopathogenic fungi,especially compound 7b,which showed 100%,80%,90%,and 90%antifungal activity(in virto)against Erysiphe graminis(***),Puccinia sorghi Schw:(P sorghi Schw.)Colletotrichum lagenarium(***),and Pseudoperonospora cubensis(P cubensis)at 300 ug/mL,*** or comparable to the positive control ***,compound 7b exhibited 85%greenhouse *** activity(in vivo)against *** even at 0.2μg/mL,equal to azoxystrobin(90%)and trifloxystrobin(90%)Meanwhile,compound 7b against P cubensis displayed 70%and 55%greenhouse inhibition activity(in vivo)at 1.56 and 0.2μg/mL,respectively,much better than those of azoxystrobin and trifloxystrobin(both 0%at 1.56 and 0.2 ug/mL).Therefore,compound 7b could be considered as the most promising fungicidal candidate for furthe ***,based on the effective concentration(ECso)against ***,the built CoMSIA model provided the useful reference for the further structural optimization design.

主 题 词：Strobilurin 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide Fungicidal activity CoMSIA model 

学科分类：081704[081704] 07[理学] 08[工学] 0817[工学-轻工类] 070303[070303] 0703[理学-化学类] 

核心收录：

D　O　I：10.1007/s40242-020-0160-9

馆 藏 号：203980498...