N-(取代噻唑-2-基)-菊酰胺类化合物的合成及生物活性研究  

Synthesis and Biological Activities of N-(Substituted-thiazole-2-yl)-chrysanthemumamide

作　　者：赵金浩[1] 周勇[1] 徐旭辉[1] 朱烈[1] 朱国念[1] 程敬丽[1] 

机构地区：[1]浙江大学农业与生物技术学院农药与环境毒理研究所,杭州310029

出　　处：《有机化学》2010年第5期719-725,共7页Chinese Journal of Organic Chemistry

基　　金：浙江省教育厅(No20050145)资助项目

摘　　要：为了寻求新颖的氨基噻唑类先导化合物,以含各种取代基的2-氨基噻唑在其氨基位置与拟除虫菊酯类农药的活性基团——菊酸采用亚结构对接的方法合成了35个N-(取代噻唑-2-基)-菊酰胺类化合物,经1HNMR,ESI-MS和元素分析对化合物的结构进行了表征.初步生物活性测定表明,化合物3d,6a,6d,4a,4b,4c和4e在600mg/L下对小菜蛾具有100%的杀虫活性,化合物3d和7c在50mg/L下对多种常见病原菌具有显著的杀菌活性,全部化合物没有明显的除草活性.In order to find new thiazole lead compounds, thirty five N-（substituted-thiazole-2-yl）-chrysanthemumamides were synthesized from five types of chrysanthemic acids with seven substituted 2- amino-thiazols. The structures of all new compounds were confirmed by ^1H NMR, MS techniques and elemental analysis. At the concentration of 600 mg/L, compounds 3d, 6a, 6d, 4a, 4b, 4c and 4e showed insecticidal activity （100%） against Plutella xylostella Linnaeus. At the concentration of 50 mg/L, compounds 3d and 7c possessed good fungicidal activity toward the tested pathogens. All compounds have shown no herbicidal activity.

关 键 词：N-取代噻唑菊酰胺 杀虫活性 杀菌活性 

分 类 号：TQ450.1[化学工程—农药化工]