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中文摘要：
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。
英文摘要：
A series of novel N-acyl-thiochromenothiazol-2-amine derivatives were designed and synthesized, furthermore, their inhibition effect on acetylcholinesterase was investigated. N-Acyl-thiochromenothiazol-2- amines were prepared from thiophenol by Hantzsch reaction, acylation reaction and substitution reaction. Moreover, their bioactivities as AChE inhibitors in vitro were measured with Ellman spectrophotometry. The results showed that most of them had a certain inhibition activity on ACHE, and the compound 10a was the best in them. The IC50 of 10a to AChE is 7.92 μmol·L^-1, and the value is better than that of rivastigmine. N-Acyl-thiochromenothiazol-2-amine derivatives showed a certain bioactivity in vitro, which were worth further investigation.
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