Design, Synthesis, and Evaluation of Fungicidal Activity of Novel Pyrazole-Containing Strobilurin Derivatives

作     者：Zesheng Hao Weibo Wang Bin Yu Xin Qi You Lv Xiaoyu Liu Haoyin Chen Tatiana A.Kalinina Tatiana V.Glukhareva Zhijin Fan Zesheng Hao;Weibo Wang;Bin Yu;Xin Qi;You Lv;Xiaoyu Liu;Haoyin Chen;Tatiana A.Kalinina;Tatiana V.Glukhareva;Zhijin Fan

作者机构：State Key Laboratory of Elemento-Organic ChemistryCollege of ChemistryNonkoi UniversityTianjin 300071China The Ural Federal University Named after the First President of Russia B.N.YeltsinYeltsin UrFU 620002EkaterinburgRussia 

出 版 物：《Chinese Journal of Chemistry》 (中国化学（英文版）)

年 卷 期：2021年第39卷第6期

页      面：1531-1537页

核心收录：

学科分类：081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0703[理学-化学] 

基　　金：the National Natural Science Foundation of China(No.31872007) the Tianjin Natural Science Foundation(No.18JCZDJC33500) the International Science&Technology Cooperation Program of China(No.2014DFR41030) the Tianjin Development Program for Innovation and Entrepreneurship 

主　　题：Drug design Strobilurins Biological activity Structure-activity relationships Cytochrome bc_(1)complex 

摘      要：In searching for novel fungicidal leads,a series of pyrazole-containing strobilurins were rationally designed,synthesized and *** indicated that compound 1-7 displayed excellent fungicidal activity against a broad spectrum of plant pathogens such as Gibberella zeae,Rhizoctonia cereolis,Sclerotinia sclerotiorum,Phytophthora infestans,Physolosporo piricola and Pellicularia sosakii with EC_(50) of 0.16,0.02,0.72,0.07,0.77 and 0.65μg/mL,respectively,which were 3-10 times more potent than the positive control azoxystrobin against the corresponding ***,like azoxystrobin and kresoxim methyl,1-7,displayed excellent protec-tive activity against *** docking validated that 1-7 and azoxystrobin would share a similar binding mode with cytochrome bc_(1) *** study demonstrates that 1-7 is a promising fungicidal candidate for further development.