Design, Synthesis, and Biological Evaluation of 5H-Thiazolo[3,2-a]pyrimidine-6-carboxylic Acid Ethyl Ester Derivatives as a Novel Series of Acetylcholinesterase Inhibitors
查看参考文献10篇
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文摘
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Acetylcholinesterase inhibitors are the most frequently prescribed anti-Alzheimer's drugs. A series of 5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid ethyl ester derivatives as the novel acetylcholinesterase inhibitors was designed based on virtual screening methods. The target compounds were synthesized with Biginelli reaction and Hantzsch-type condensation of dihydropyrimidines with substituted phenacyl chlorides, and were characterized with elemental analysis, IR, MS, ~1H NMR, and ~(13)C NMR. The biological evaluation against human acetylcholinesterase in vitro indicated all the target compounds show more than 50% inhibition at 10 μmol/L by means of the Ellman method. The results provide a starting point for the development of novel drugs to treat Alzheimer's disease and lay the foundation of searching for improved acetylcholinesterase inhibitors with the novel scaffolds. |
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来源
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Chemical Research in Chinese Universities
,2009,25(3):332-337 【核心库】
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关键词
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Acetylcholinesterase inhibitor
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Docking screening
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Heterocycle
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Biological activity
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5H-Thiazolo[3
;
2-a] pyrimidine-6-carboxylic acid ethyl ester derivative
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地址
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1.
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Liaoning, Shenyang, 110016
2.
Department of Biochemistry, The Chinese University of Hong Kong
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语种
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英文 |
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文献类型
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研究性论文 |
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ISSN
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1005-9040 |
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学科
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化学 |
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文献收藏号
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CSCD:3684013
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