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本文设计、合成了一类全新结构类型的N-酰基-硫色烯并噻唑-2-胺类化合物,并考察了这些化合物对乙酰胆碱酯酶活性的抑制作用。以苯硫酚为起始原料,经Hantzsch、酰化和取代反应合成了N-酰基-硫色烯并噻唑-2-胺类化合物;利用Ellman分光光度法考察了它们对乙酰胆碱酯酶(AChE)的体外抑制活性。试验结果表明目标化合物均具有一定的AChE抑制活性,其中化合物10a抑制活性最好,其IC50达到了7.92μmol·L-1,优于对照药利斯的明。N-酰基-硫色烯并噻唑-2-胺类化合物对乙酰胆碱酯酶具有较好的抑制活性,值得进一步深入研究。
In this paper, we designed and synthesized a new class of N-acyl-thienolethiazol-2-amine compounds and investigated the inhibitory effect of these compounds on acetylcholinesterase activity. N-acyl-sulfur chromen thiazol-2-amine compounds were synthesized by the reaction of Hantzsch, acylation and substitution with thiophenol as the starting material. Their effects on acetylcholinesterase (AChE) activity were investigated by Ellman spectrophotometry. In vitro inhibitory activity. The experimental results showed that the target compounds all had certain AChE inhibitory activity. Among them, compound 10a showed the best inhibitory activity with an IC50 of 7.92 μmol·L-1, which was better than that of the control drug. N-acyl-thienolethiazol-2-amine compounds have good inhibitory activity on acetylcholinesterase, which deserves further study.