Development of Cholinesterase Inhibitors Using (a)-Lipoic Acid-benzyl Piperazine Hybrid Molecules 


Vol. 34,  No. 11, pp. 3322-3326, Nov.  2013
10.5012/bkcs.2013.34.11.3322


PDF
  Tumbnail

  Abstract

A series of hybrid molecules between (α)-lipoic acid (ALA) and benzyl piperazines were synthesized and their in vitro cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibitory activities were evaluated. Even though the parent compounds did not show any inhibitory activity against cholinesterase (ChE), all hybrid molecules showed BuChE inhibitory activity. Some hybrid compounds also displayed AChE inhibitory activity. Specifically, ALA-1-(3-methylbenzyl)piperazine (15) was shown to be an effective inhibitor of both BuChE (IC50 = 2.3 ± 0.7 μM) and AChE (IC50 = 30.31 ± 0.64 μM). An inhibition kinetic study using compound 15 indicated a mixed inhibition type. Its binding affinity (Ki) value to BuChE is 2.91 ± 0.15 μM.

  Statistics
Cumulative Counts from November, 2022
Multiple requests among the same browser session are counted as one view. If you mouse over a chart, the values of data points will be shown.


  Cite this article

[IEEE Style]

B. Kim, S. Lee, M. Jang, M. Shon, J. H. Park, "Development of Cholinesterase Inhibitors Using (a)-Lipoic Acid-benzyl Piperazine Hybrid Molecules," Bulletin of the Korean Chemical Society, vol. 34, no. 11, pp. 3322-3326, 2013. DOI: 10.5012/bkcs.2013.34.11.3322.

[ACM Style]

Beom-cheol Kim, Seung-hwan Lee, Mi Jang, MinYoung Shon, and Jeong Ho Park. 2013. Development of Cholinesterase Inhibitors Using (a)-Lipoic Acid-benzyl Piperazine Hybrid Molecules. Bulletin of the Korean Chemical Society, 34, 11, (2013), 3322-3326. DOI: 10.5012/bkcs.2013.34.11.3322.

Search
(IN TITLE, AUTHOR, ABSTRACT,KEYWORDS)

Advanced Search ▼

POPULAR KEYWORDS
(TOP 10 KEYWORDS)

Recent Publications
(LAST 3 YEARS)

ISSN(Print) 0253-2964
ISSN(Online) 1229-5949