1451180-84-9Relevant academic research and scientific papers
Synthesis of selective butyrylcholinesterase inhibitors coupled between α-lipoic acid and polyphenols by using 2-(piperazin-1-yl)ethanol linker
Yeun, Go Heum,Lee, Seung Hwan,Lim, Yong Bae,Lee, Hye Sook,Won, Moo-Ho,Lee, Bong Ho,Park, Jeong Ho
, p. 1025 - 1029 (2013/07/28)
In the previous paper (Bull. Korean Chem. Soc., 2011, 32, 2997), the hybrid molecules between a-lipoic acid (ALA) and polyphenols (PPs) connected with neutral 2-(2-aminoethoxy)ethanol linker (linker-1) showed new biological activity such as butyrylcholinesterase (BuChE) inhibition. In order to increase the binding affinity of the hybrid compounds to cholinesterase (ChE), the neutral 2-(2-aminoethoxy)ethanol (linker 1) was switched to the cationic 2-(piperazin-1-yl)ethanol linker (linker 2). The IC50 values of the linker-2 hybrid molecules for BuChE inhibition were lower than those of linker-1 hybrid molecules (except 9-2) and they also had the same great selectivity for BuChE over AChE (> 800 fold) as linker-1 hybrid molecules. ALA-acetyl caffeic acid (10- 2, ALA-AcCA) was shown as an effective inhibitor of BuChE (IC50 = 0.44 ± 0.24 μM). A kinetic study using 7- 2 showed that it is the same mixed type inhibition as 7-1. Its inhibition constant (Ki) to BuChE is 4.3 ± 0.09 μM.
