Abstract
A series of photoinduced palladium-catalyzed 1,3-diene-selective fluoroalkylamination derivatives was ra-tionally synthesized based on diversity-oriented synthesis via cross coupling of 1,3-dienes,amines and fluoroalkyl iodides.The reaction featured good function group tolerance and a broad substrate scope,which could be extended to the late-stage modification of bioactive molecules.Bactericidal activity of all the compounds against Xanthomonas oryzae pv.oryzae(Xoo)was evaluated.Among them,compound E14 showed significant activity against Xanthomonas oryzae pv.oryzae(Xoo)with half maximal effective con-centration(EC50)value of 6.61μmol/mL.In pot experiments,the results showed that E14 could control rice bacterial blight with protective and curative efficiencies of 37.5％and 63.2％at 200μg/mL,respec-tively.Additionally,a plausible mechanism for antibacterial behavior of E14 was proposed by electron microscopy,flow cytometry,reactive oxygen species detection,and biofilm assay.In current work,it can promote the development of photoinduced palladium-catalyzed 1,3-diene-selective fluoroalkyl amination compounds as prospective antibacterial agent bearing an intriguing mode of action.
基金项目
国家自然科学基金(32072450)
National science Fund for Distinguished Young Scholars of Guangdong Province(2021B1515020107)
International Science and Technology Cooperation Program in Guangdong(2020A0505100048)
International Science and Technology Cooperation Program in Guangdong(2022A0505050060)
NETL
NSTL
维普
万方数据