含芳烷胺他克林衍生物的合成与活性研究
首发时间:2009-01-16
摘要:根据AChE具有双活性中心的结构特点,以他克林作为结合外周位点的片段,以芳烷基胺作为结合催化位点的片段,采用酰胺键进行连接,合成了8个含芳烷胺他克林衍生物6a-6h,结构经IR、1H-NMR、MS确证,初步的体外AChE、BChE抑制活性试验表明,大部分化合物都显示一定的抑制AChE活性,其中6f的IC50为0.35μmol/L,而所有化合物基本都显示弱的BChE抑制活性。
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The synthesis and evaluation of tacrine derivatives containing aromatic alkyl amine
Abstract:The X-ray structure of AChE reveals that it contains peripheral anionic site and central site. Tacrine (interacting with the peripheral site) and aromatic alkyl amine moiety (interacting with the central site) were chosen and linked with amide chain. Eight tacrine derivatives were synthesized and the structure were confirmed by IR、1H-NMR、MS. The results of AChE and BChE evaluation showed that most of them exhibit middle AChE inhibitory activity, the most potent compound is 6f (IC50 = 0.35μmol/L), while all the compounds exhibit low inhibitory activity.
Keywords: Tacrine derivatives synthesis AChE inhibitory activities.
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No.2801839116312320****
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