Design,Synthesis And Biological Evaluation Of Novel Nematicides

Three series of novel nematicides were designed and synthesized based on some nematicidal structural fragments,their structures were confirmed by 1H NMR,13C NMR and high resolution mass spectroscopy(HRMS).Their bioactivities were evaluated and some of the target compounds exhibited good nematicidal activities,which might be optimized as potential lead compounds.1).33 pyazole-amide derivatives containg 1,2,3-triazoles were designed and synthesized via click chemistry in one-pot reaction,and their by-pruducts were studied.Most of the synthesized compounds showed excellent inhibitory activities against Meloidogyne incongnita at 25 mg/L,IPP196811,IPP196813-IPP196816,IPP196819-IPP196821 exhibited 100%inhibition at 20 mg/L.Also,IPP196831 and IPP196834 displayed 100%inhibition at 10 mg/L.Bioassays indicated that electron-donating group or fluorine-substitued in benzene ring played a positive role in promoting their nematicidal activities against Meloidogyne incongnita.2).22 novel biaryl lactams were designed and synthesized via Smiles rearrangement or direct cyclization.Bioassays showed that the novel biaryl lactams exhibited moderate inhibitory activities against Meloidogyne incongnita at 25 mg/L.Among the tested compounds,IPP196611 and IPP196615 displayed more than 90%inhibition at 25 mg/L.Also,the reaction condition was optimized,the scope of substates and the mechanism of the reaction was investigated.3)Chorismate mutase is one of the important target of nematode,carvacrol and its analoges exhibited inhibitory activities against chorismate mutase.25 novel carvacrol derivatives were designed and synthesized based on this result.Bioassays showed that some of the target compounds exhibited moderate to high activities against Meloidogyne incongnita.Among the tested compounds,IPP196861 and IPP196873 displayed 93.9%and 100%inhibition rate at 10 mg/L,respectively.