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Synthesis and AchE inhibitory activity of 2-phenoxy-indan-1-one derivatives
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- Author:
- No author available
- Journal Title:
- ACTA PHARMACEUTICA SINICA
- Issue:
- 2
- DOI:
- 10.3321/j.issn:0513-4870.2006.02.004
- Key Word:
- 苯氧茚酮类衍生物;合成;AchE抑制活性;BchE抑制活性
Abstract： 目的设计、合成新型的AchE抑制剂.方法在K2CO3和乙腈存在下,将2-溴-5,6-二甲氧基-1-茚酮与多种胺烷基苯酚缩合得到一系列苯氧茚酮类衍生物,并采用改进的Ellman方法研究它们的体外AchE和BchE抑制活性.结果合成了16个未见文献报道的化合物8a～p,结构经IR,1H NMR,MS及元素分析确证.初步体外AchE,BchE抑制活性试验表明,绝大部分化合物都显示出良好的抑制AchE活性,其中8h的IC50为50.0 nmol·L-1,与石杉碱甲相近(IC50=53.0 nmol·L-1);而所有化合物基本都无BchE抑制活性.结论该类衍生物具有较强的AchE抑制活性,有进一步研究的价值.
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