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 

机构地区：[1]State Key Laboratory of Elemento-Organic Chemistry,College of Chemistry,Nonkoi University,Tianjin 300071,China [2]The Ural Federal University Named after the First President of Russia B.N.Yeltsin,Yeltsin UrFU 620002,Ekaterinburg,Russia

出　　处：《Chinese Journal of Chemistry》2021年第6期1531-1537,共7页中国化学（英文版）

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.

摘　　要：In searching for novel fungicidal leads,a series of pyrazole-containing strobilurins were rationally designed,synthesized and charac-terized.Bioassay 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 pathogens.Moreover,like azoxystrobin and kresoxim methyl,1-7,displayed excellent protec-tive activity against P.sorghi.Molecular docking validated that 1-7 and azoxystrobin would share a similar binding mode with cytochrome bc_(1) complex.This study demonstrates that 1-7 is a promising fungicidal candidate for further development.

关 键 词：Drug design STROBILURINS Biological activity Structure-activity relationships Cytochrome bc_(1)complex 

分 类 号：O62[理学—有机化学]