In recent years,the damage caused by soil nematodes has become increasingly serious;however,the varieties and structures of the nematicides available on the market are deficient.Fluopyram,a succinate dehydrogenase inh...In recent years,the damage caused by soil nematodes has become increasingly serious;however,the varieties and structures of the nematicides available on the market are deficient.Fluopyram,a succinate dehydrogenase inhibitor(SDHI)fungicide developed by Bayer AG in Germany,has been widely used in the prevention and control of soil nematodes due to its high efficiency and novel mechanism of action.In this paper,two series of novel target compounds were designed and synthesized with nematicidal and fungicidal fluopyram as the molecular skeleton in order to introduce sulfide and sulfone substructures.The structures were identified and characterized by 1H nuclear magnetic resonance(NMR),13C NMR,and high-resolution mass spectrometer(HRMS).The bioassays revealed that most of the compounds showed excellent nematicidal activities at 200 lgmL-1 in comparison with fluopyram,while the nematode mortality rate dropped sharply at 100μg·mL-1,except for compounds I-11 and II-6.In terms of fungicidal activity,compound I-9 was discovered to have an excellent inhibitory rate,and a molecular docking simulation was performed that can provide important guidance for the design and exploration of efficient fungicidal lead compounds.展开更多
基金This work was financially supported by the Natural Science Foundation of Shandong Province,China(ZR2017BC053)the Doctoral Research Startup Foundation of Liaocheng University(318051625).
文摘In recent years,the damage caused by soil nematodes has become increasingly serious;however,the varieties and structures of the nematicides available on the market are deficient.Fluopyram,a succinate dehydrogenase inhibitor(SDHI)fungicide developed by Bayer AG in Germany,has been widely used in the prevention and control of soil nematodes due to its high efficiency and novel mechanism of action.In this paper,two series of novel target compounds were designed and synthesized with nematicidal and fungicidal fluopyram as the molecular skeleton in order to introduce sulfide and sulfone substructures.The structures were identified and characterized by 1H nuclear magnetic resonance(NMR),13C NMR,and high-resolution mass spectrometer(HRMS).The bioassays revealed that most of the compounds showed excellent nematicidal activities at 200 lgmL-1 in comparison with fluopyram,while the nematode mortality rate dropped sharply at 100μg·mL-1,except for compounds I-11 and II-6.In terms of fungicidal activity,compound I-9 was discovered to have an excellent inhibitory rate,and a molecular docking simulation was performed that can provide important guidance for the design and exploration of efficient fungicidal lead compounds.
