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

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.