取代苯甲醛缩氨基硫脲(脲、硝基胍)类化合物的合成及其对小菜蛾酪氨酸酶的抑制活性  

Synthesis of substituted benzylidene hydrazinecarbothioamide (hydrazinecarboxamide,nitrohydrazinecarboximidamide) and their inhibitory activity on tyrosinase of diamondback moth Plutella xylostella (L.)

作　　者：王振[1] 董玮[2] 徐焱[1] 梁沛[2] 杨新玲[1] 

机构地区：[1]中国农业大学理学院/农业部农药化学与应用重点开放实验室,北京100193 [2]中国农业大学农学与生物技术学院,北京100193

出　　处：《农药学学报》2010年第3期264-268,共5页Chinese Journal of Pesticide Science

基　　金：国家高技术研究发展计划(“863”计划)项目(2006AA10A201)

摘　　要：酪氨酸酶是昆虫生长发育过程中的一个关键性酶,控制酪氨酸酶的活性即可调节昆虫的生长行为。以苯甲醛缩氨基硫脲为母体化合物,通过变换硫脲结构片段,设计了18个结构类似的苯甲醛缩氨基硫脲(脲、硝基胍)类化合物,以取代苯甲醛、氨基硫脲、水合肼等为原料经1～2步反应合成了目标化合物,其结构通过红外、核磁共振氢谱、质谱(ESI)表征。生物活性测试结果表明,硫脲类化合物对小菜蛾酪氨酸酶的抑制活性明显高于脲(硝基胍)类化合物,说明硫脲结构的存在对化合物的活性有利。Tyrosinase is a key enzyme in the growth and development of insect.The development of insect can be affected by regulating its tyrosinase activity.Eighteen substituted benzylidene hydrazinecarbothioamide (hydrazinecarboxamide,nitrohydrazinecarboximidamide) compounds were designed based on changing the thiourea structure fragment of parent compound benzylidene hydrazinecarbothioamide.The title compounds were synthesized from the starting materials of substituted benzaldehyde,thiosemicarbazide,hydrazine hydra...

关 键 词：硫脲(脲 硝基胍) 合成 酪氨酸酶 生物活性 

分 类 号：O625.4[理学—有机化学]