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

作　　者：熊传武 张雪鹏[2] 罗喜爱 刘奕奕 刘建兵[2] XIONG Chuan-wu;ZHANG Xue-peng;LUO Xi-ai;LIU Yi-yi;LIU Jian-bing(Department of Pharmacy,Hunan University of Medicine,Huaihua 418000,China;Key Laboratory of the Assembly and Application of Organic Functional Molecules,Key Laboratory of Chemical Biology and Traditional Chinese Medicine Research,Ministry of Education,National and Local Joint Engineering Laboratory for New Petro-Chemical Materials and Fine Utilization of Resources,Hunan Normal University,Changsha 410081,China;Electric Power Research Institute,State Grid Hunan Electric Power Co.,Ltd,Changsha 410007,China)

机构地区：[1]湖南医药学院药学院,中国怀化418000 [2]湖南师范大学石化新材料与资源精细利用国家地方联合工程实验室,化学生物学及中药分析省部共建教育部重点实验室,有机功能分子组装与应用重点实验室,中国长沙410081 [3]国网湖南省电力有限公司电力科学研究院,中国长沙410007

出　　处：《湖南师范大学自然科学学报》2021年第5期116-123,共8页Journal of Natural Science of Hunan Normal University

基　　金：湖南省自然科学基金资助项目(2020JJ6048);湖南省教育厅资助科研项目(17C1137);湖南省教育厅资助重点科研项目(20A327)。

摘　　要：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.

关 键 词：苯甲酰脲 先导化合物 活性亚结构拼接法 5-氨基噻唑 生物活性 

分 类 号：TQ453.2[化学工程—农药化工]