Development of Selective Butyrylcholinesterase Inhibitors Using (R)-Lipoic Acid-Polyphenol Hybrid Molecules

A series of hybrid molecules between (R)-lipoic acid (ALA) and the acetylated or methylated polyphenol compounds were synthesized and their in vitro cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibition activities were checked. The IC_50 values of all hybrid molec...

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Bibliographic Details
Published in:Bulletin of the Korean Chemical Society 2011, 32(8), , pp.2997-3002
Main Authors: Woo, Yeun-Ji, Lee, Bo-Hyun, Yeun, Go-Heum, Kim, Hyun-Ju, Ko, Jang-Myoun, Won, Moo-Ho, Lee, Bong-Ho, Park, Jeong-Ho
Format: Article
Language:English
Subjects:
화학
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Summary:A series of hybrid molecules between (R)-lipoic acid (ALA) and the acetylated or methylated polyphenol compounds were synthesized and their in vitro cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibition activities were checked. The IC_50 values of all hybrid molecules for a BuChE inhibition were lower than those of the single parent compounds. Specifically, ALA-acetyl protected caffeic acid (11,ALA-AcCA) was shown as an effective inhibitor of BuChE (IC_50 = 0.5 ± 0.2 μM) and also had a great selectivity for BuChE over AChE (more than 800 fold). Inhibition kinetic study indicated that 11 is a mixed inhibition type. Its binding affinity (Ki) value to BuChE is 1.52 ± 0.18 μM. KCI Citation Count: 13
ISSN:0253-2964
1229-5949
DOI:10.5012/bkcs.2011.32.8.2997