文献类型：期刊文献

英文题名：Azo-incorporating Increases Inhibitory Activity of Succinate Dehydrogenase

作者：Fu, Wen[1];Hu, Xinyue[1];Yuan, Qinglong[1];Sun, Xujuan[1];Xu, Zhiping[1];Zhang, Yang[1];Cheng, Jiagao[1];Ye, Yonghao[2];Li, Zhong[1,3];Shao, Xusheng[1,3]

机构：[1]East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China;[2]Nanjing Agr Univ, Coll Plant Protect, State & Local Joint Engn Res Ctr Green Pesticide, Nanjing 210095, Peoples R China;[3]East China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China

年份：2021

卷号：69

期号：45

起止页码：13448

外文期刊名：JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY

收录：;EI(收录号：20214711196577);WOS:【SCI-EXPANDED(收录号:WOS:000727379700001)】；

基金：This work was financially supported by National Natural Science Foundation of China (nos. 21877039 and 32072441), National Key Research and Development Program of China (2018YFD0200100), and Innovation Program of Shanghai Municipal Education Commission (2017-01-07-00-02-E00037).

语种：英文

外文关键词：azobenzene; activity; fungicide; succinate dehydrogenase

摘要：Diversity of pesticide discovery provided a solution to resistance. Here, we presented a strategy of azo-incorporating to promote the diverse developments of fungicide. A series of novel fungicides were synthesized by incorporating azobenzene derivatives into fluxapyroxad. Much better in vitro fungicidal activity increases for compound 9d were observed compared to the positive control, fluxapyroxad against Botrytis cinerea and Rhizoctonia solani. Compound 9d (IC50 = 0.03 mu M) also had a great enzyme-inhibiting activity increase toward succinate dehydrogenase in comparison with fluxapyroxad (IC50 = 4.40 mu M). A comparatively equivalent biological activity was observed between compounds 8a and 9d. SEM analysis helped us to observe clearly the morphology of the fungi before and after active ingredient delivery. Our results of molecular docking analysis, fluorescence quenching analysis, and enzymatic assays demonstrated that compound 8a and 9d act on SDH. An increase in inhibitory activity could be occurring after incorporation of azobenzene, which provided a new strategy for molecular design in pesticide discovery.