设计、合成和评价氨甲酰基修饰的(-)-N(1)-苯乙基降烟碱衍生物作为选择性丁酰胆碱酯酶抑制剂。
Design, synthesis and evaluation of carbamate-modified (-)-N(1)-phenethylnorphysostigmine derivatives as selective butyrylcholinesterase inhibitors.
机构信息
Department of Neuroscience for Drug Discovery, Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Yoshida-Shimoadachi-cho, Sakyo-ku, Kyoto 606-8501, Japan.
出版信息
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1721-3. doi: 10.1016/j.bmcl.2010.01.035. Epub 2010 Jan 20.
PMID:20137941
Abstract
We synthesized carbamate-modified (-)-N(1)-phenethylnorphysostigmine derivatives 3a-u and evaluated their anti-cholinesterase activities. In vitro evaluation showed that cyclohexylmethylcarbamate derivative 3u potently and selectively inhibits butyrylcholinesterase.
摘要
我们合成了氨基甲酸酯修饰的（-）-N(1)-苯乙基降烟碱衍生物 3a-u，并评估了它们的抗胆碱酯酶活性。体外评价表明，环己基甲基氨基甲酸酯衍生物 3u 对丁酰胆碱酯酶具有强大且选择性的抑制作用。
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