Synthesis And Investigation Of Insecticidal Activity Of Nereistoxin Compounds

The growth of global population and climate change make the situation of food security not so optimistic, and the pesticides make a significant contribution to protect the harvest of agriculture, elimination of hunger and poverty, ensure people live a healthy and happy life. The Bionic pesticides were particularly concerned about its property of low toxicity and residue, environmental friendly, high efficient and broad-spectrum insecticide et al. As a kind of commercial valuable bionic pesticide, nereistoxin pesticides are developed from nereistoxin, a kind of toxic active substances inside of the sea animal named lumbriconereis heteropoda. Nereistoxin pesticides have been drawn attention by people owing to its advantages of low toxicity, low residue and environmentally friendly. However, long term application of pesticides lead the pests have resistance, nereistoxin pesticides also encount the same situation.So this study aims to reach for compounds with excellent insecticidal effect and the preparation methods by structure modification of nereistoxin.The design, synthesis, characterization, insecticidal activity and the relationship between structure and biological activity of nereistoxin compounds were studied in this paper. Twenty-one unreported nereistoxin compounds were synthesized with serinol, thiophenol derivants, phenol derivants and2-amino-5-methylthiazole as raw material. All compounds were identified by1H and13C nuclear magnetic resonance (NMR), IR, and MS.Preliminary bioassays indicated the target compounds exhibited good insecticide activities against Panonychus citri at1000ppm, the mortality rates of eleven target compounds are100%, and mortality rates of rest is all above90%. The structures change has no significant effect on the insecticide activity in this assay. But the transformation of structures lead to different insecticide activities against Panonychus citri at2000ppm. The activities of PJW12, PJW15, PJW20are much higher than Monosultap’s, seven target compounds equivalent to it’s, and the rest evaluated are inferior.