Trifluoromethyl pyridine(TFMP)motif is commonly discovered in structures of active pharmaceuticals.Flonicamid,characterized by the TFMP moiety,is well known as a prodrug in the knockdown of pests.The azobenzene-modifi...Trifluoromethyl pyridine(TFMP)motif is commonly discovered in structures of active pharmaceuticals.Flonicamid,characterized by the TFMP moiety,is well known as a prodrug in the knockdown of pests.The azobenzene-modified TFMP derivatives have been previously reported with excellent insecticidal activities.Herein,twenty-one TFMP derivatives were designed by the introduction of carbonyl-bridged aryl groups and synthesized via a one-step synthesis using Flonicamid as the starting material.The structure-activity relationships of these compounds were well analyzed and discussed.A molecular docking study and calcium ion concentration analysis indicated that compound FC13 could have interacted with the nicotinamidase enzyme,which further influenced the Ca^(2+)influx.展开更多
基金supported by National Natural Science Foundation of China(32472610,32402439,32072441)National Key Research and Development Program of China(2018YFD0200100)+3 种基金Innovation Program of Shanghai Municipal Education Commission(2017-01-07-00-02-E00037)Tobacco and Health funding program(2022539200340111)Shanghai Frontiers Science Center of Optogenetic Techniques for Cell Metabolism(Shanghai Municipal Education Commission)the project of National Key Laboratory of Green Pesticide/Key Laboratory of Green Pesticide and Agricultural Bioengineering,Ministry of Education,Guizhou University(SKL-GPL-KF202405).
文摘Trifluoromethyl pyridine(TFMP)motif is commonly discovered in structures of active pharmaceuticals.Flonicamid,characterized by the TFMP moiety,is well known as a prodrug in the knockdown of pests.The azobenzene-modified TFMP derivatives have been previously reported with excellent insecticidal activities.Herein,twenty-one TFMP derivatives were designed by the introduction of carbonyl-bridged aryl groups and synthesized via a one-step synthesis using Flonicamid as the starting material.The structure-activity relationships of these compounds were well analyzed and discussed.A molecular docking study and calcium ion concentration analysis indicated that compound FC13 could have interacted with the nicotinamidase enzyme,which further influenced the Ca^(2+)influx.
