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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 35, Number 6
BKCSDE 35(6)
June 20, 2014 

Development of Cholinesterase Inhibitors using 1-Benzyl Piperidin-4-yl (α)-Lipoic Amide Molecules
Seung-hwan Lee, Beom-cheol Kim, Jae-kwan Kim, Hye Sook Lee, Min Young Shon*, Jeong Ho Park*
Molecular hybridization, (α)-Lipoic acid, 4-Amino-1-benzyl piperidines, Cholinesterase inhibitors
A series of hybrid molecules between (α)-lipoic acid (ALA) and 4-amino-1-benzyl piperidines were synthesized and their in vitro cholinesterase (acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)) inhibitory activities were evaluated. Even though the parent compounds did not exhibit any inhibitory activity against cholinesterase (ChE) with the exception of compound 14 (IC50 = 255.26 ± 4.41 against BuChE), all hybrid molecules demonstrated BuChE inhibitory activity. Some hybrid compounds also displayed AChE inhibitory activity. Specifically, compound 17 was shown to be an effective inhibitor against both AChE (IC50 = 1.75 ± 0.30 μM) and BuChE (IC50 = 5.61 ± 1.25 μM) comparable to galantamine (IC50 = 1.7 ± 0.9 μM against AChE and IC50 = 9.4 ± 2.5 μM against BuChE). Inhibition kinetic studies using compound 17 indicated a mixed inhibition type for AChE and a noncompetitive inhibition type for BuChE. Its binding affinity (Ki) values to AChE and BuChE were 3.8 ± 0.005 μM and 7.0 ± 0.04 μM, respectively.
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