3,5-二取代- 1,2,4-噁二唑类衍生物的合成及生物活性

目的]为了寻找具有良好生物活性的噁二唑类衍生物。方法]以苯甲腈为原料,经加成、脱水环化等反应设计合成了一系列未见文献报道的噁二唑类衍生物,并对目标化合物进行了生物活性测试。结果]其结构通过1H NMR、13C NMR和H RMS图谱得以确证。初步生物活性测试结果显示:部分目标化合物在质量浓度200 mg/L下对南方根结线虫有较好的抑制活性,其中化合物5f、6a、6b和6e对线虫的抑制率达到90%以上,尤其化合物4a、4d对线虫的抑制率达到100%,另外部分目标化合物对南方根结线虫和小菜蛾幼虫都具有一定的抑制活性。结论]该类结构具有较好的生物活性,有进一步优化的潜力。

Synthesis and Biological Activity Studies of 3,5-Disubstituted-1,2,4-oxadiazole Derivatives

Aims]This study aims to find the oxadiazole derivatives with high biological activity.Methods]A series of oxadiazole derivatives were synthesized from benzonitrile by reactions addition,dehydration cyclization etc and the biological activity of the target compounds was tested.Results]The structure was confirmed by 1H NMR,13C NMR and H RMS spectra.The results of preliminary bioassay showed that some of the target compounds had a good inhibitory activity on Meloidogyne incognita at a concentration of 200 mg/L,in which the inhibition rates of 5f,6a,6b and 6e were over 90%,and the inhibition rates of 4a and 4d were even 100%.It was also found that some target compounds have inhibitory activity against both Plutella xylostella and M.incognita.Conclusions]This type of structure has the potential for further optimization due to good biological activity.