含氟N,N'-二芳基异硫脲的合成及昆虫β-N-乙酰己糖胺酶抑制活性研究  

Synthesis and Insect β-N-acetyl-D-hexosaminidase Inhibitory Activities of Fluorine-containing N,N'-diarylisothiourea

作　　者：施倩[1] 刘鹏飞[1] 刘田[2] 杨青[2] 徐晓勇[1] 

机构地区：[1]上海化学生物学重点实验室华东理工大学药学院,上海200237 [2]大连理工大学生物科学实验室,辽宁大连116024

出　　处：《现代农药》2011年第1期16-20,23,共6页MODERN AGROCHEMICALS

基　　金：上海市科委(073919107;09391911800);上海市教委项目(B507)

摘　　要：β-N-乙酰己糖胺酶是几丁质代谢过程中一种重要的酶,已被确定为医药和农药的潜在靶标。本文合成了16个未见文献报道的含氟N,N'-二芳基异硫脲,并测定了对β-N-乙酰己糖胺酶OfHex1和OfHex2的抑制活性,酶活性测试表明对OfHex2显示出一定的抑制效果。β-N-acetyl-D-hexosaminidase,which has been identified as potential pharmaceutical and pesticide target,is an important enzyme of chitin metabolism.In this article,we synthesized a series of fluorine-containing N,N＇-diaryliso-thiourea compounds and determined their inhibitory activity on β-N-acetyl-D-hexosaminidase OfHex1 and OfHex2,which were isolated,purified and characterized from the fifth instar larva integument of the Asian corn borer,Ostrinia furnacalis（Guenée）.The primary test suggested that they showed certain inhibitory activity against OfHex2.

关 键 词：合成 β-N-乙酰己糖胺酶 结构修饰 

分 类 号：TQ453.2[化学工程—农药化工]