| Literature DB >> 26943478 |
Nisachon Khunnawutmanotham1, Nitirat Chimnoi2, Patchreenart Saparpakorn3, Supanna Techasakul4.
Abstract
A series of scopoletin derivatives incorporated with the pyridinium moiety was synthesized and evaluated for their acetylcholinesterase (AChE) inhibitory activity by the colorimetric Ellman's method. A 2-fluorobenzylpyridinium derivative was the most potent among the tested compounds, with an IC50 value of 0.215±0.015μM, which was greatly improved from that of scopoletin. Docking studies revealed that the scopoletin portion of the mentioned compound was bound to the peripheral anionic site of the AChE, whereas the N-benzylpyridinium residue to the catalytic anionic site.Entities:
Keywords: Acetylcholinesterase inhibitor; Pyridinium derivatives; Scopoletin; Synthesis
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Year: 2015 PMID： 26943478 DOI： 10.1016/j.bioorg.2015.12.002
Source DB: PubMed Journal: Bioorg Chem ISSN： 0045-2068 Impact factor: 5.275