新型5-氨基噻唑苯甲酰脲类化合物的合成及生物活性

Synthesis and Biological Activities of New Benzoylureas Containing 5-Aminothiazole Ring

以商品化的苯甲酰脲作先导化合物,基于活性亚结构拼接法,将5-氨基噻唑单元替换原有的苯胺部分,成功制备了13个未见文献报道的新化合物,通过^(1)H NMR、^(13)C NMR、IR、MS以及元素分析确认了所有化合物的结构。离体生物活性结果显示,大部分化合物具有优异的杀虫活性:当浓度为200 mg·L^(-1)时,化合物1g对棉铃虫和玉米螟的杀虫活性均为100%;当浓度为10 mg·L^(-1)时,化合物1c,1e,1i及1k对蚊幼虫的杀虫活性为100%。

Employing commercial benzoyurea as the leading compound,we successfully prepared 13 new compounds by replacing the original aniline part with 5-aminothiazole unit based on active substructure splices.The structures of all these new compounds were confirmed by ^(1)H NMR,^(13)C NMR,IR,MS and elemental analysis.Our in vitro biological activity test results showed that most of the compounds exhibited excellent insecticidal activity.When its concentration was 200 mg·L^(-1),Compound 1 g had 100%insecticidal activity against cotton bollworm and corn borer.When their concentration was 10 mg·L^(-1),Compounds 1 c,1 e,1 i and 1 k displayed 100%insecticidal activity against mosquito larvae.