新型三嗪酮硫醚衍生物的合成及生物活性

Synthesis and biological activities of novel triazone thioether derivatives

[目的]为了发现具有更高生物活性的新化合物。[方法]采用活性结构拼接法将硫醚片段引入吡蚜酮结构中,设计并合成了10个三嗪酮硫醚衍生物,并对其进行了杀虫活性和抑菌活性测试。[结果]目标化合物的结构经^(1)H NMR、^(13)C NMR和HRMS分析确证。部分化合物在600 mg/L下对蚜虫和小菜蛾防效≥80%,在50 mg/L下对油菜菌核菌和苹果轮纹菌的抑菌率高于70%;化合物5j在10 mg/L下对蚊幼虫的致死率为70%。[结论]此类化合物具有一定的杀虫和杀菌效果,值得进一步研究。

[Aims]This study aims to discover novel compounds with high biological activities.[Methods]Thioether fragments were introduced into triazone by active structure splicing method to synthesize 10 triazone thioether derivatives.The insecticidal and fungicidal activities were tested.[Results]The structures of the target compounds were confirmed by ^(1)H NMR,^(13)C NMR and HRMS.Some compounds showed≥80%control efficacy against Aphis craccivora and Plutella xylostella,showed more than 70%inhibition against Sclerotinia sclerotiorum and Physalospora piricol,the lethal rate of compound 5j against mosquito larvae was 70%.[Conclusions]The target compounds exhibit certain insecticidal and fungicidal activities and are worth further study.