<i>N</i>-酰基-4-苯基噻唑-2-胺类衍生物的设计、合成及其乙酰胆碱酯酶抑制活性的研究

N-酰基-4-苯基噻唑-2-胺类衍生物的设计、合成及其乙酰胆碱酯酶抑制活性的研究

摘要: 以α-溴代苯乙酮作为原料，经过3步反应，合成了N-酰基-4-苯基噻唑-2-胺类化合物。采用Ellman分光光度法测试了化合物对乙酰胆碱酯酶的体外抑制活性，结果表明，目标化合物具有一定的乙酰胆碱酯酶抑制活性，其中化合物8c的抑制活性最好，其IC₅₀达到了0.51 μmol·L^-1，优于利斯的明和石杉碱甲。N-酰基-4-苯基噻唑-2-胺对乙酰胆碱酯酶的抑制活性值得进一步研究。

Abstract: N-Acyl-4-phenylthiazole-2-amines were designed and synthesized, moreover their effects onacetylcholinesterase activities were tested.N-Acyl-4-phenylthiazole-2-amines were prepared from substituted 2-bromo-1-acetophenones by three steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro.The results showed that the target compounds had a certain inhibitory activity on AChE in vitro.Among them, 8c was the best, and IC₅₀ of 8c was 0.51 μmol·L^-1, better than that of rivastigmine and Huperzine-A.The inhibitory activities of N-acyl-4-phenylthiazole-2-amines on acetylcholinesterase are worth while to be further studied.