논문 국내 국내전문학술지(KCI급) SYNTHESIS OF SELECTIVE BUTYRYLCHOLINESTERASE INHIBITORS COUPLED BETWEEN ALPHA-LIPOIC ACID AND POLYPHENOLS BY USING 2-(PIPERAZIN-1-YL)ETHANOL LINKER
- 학술지 구분 국내전문학술지(KCI급)
- 게재년월 2013-04
- 저자명 WON, MH (WON, MOO-HO),PARK, JH (PARK, JEONG HO),LEE, BH (LEE, BONG HO)공동(참여),LIM, YB (LIM, YONG BAE),LEE, SH (LEE, SEUNG HWAN),YEUN, GH (YEUN, GO HEUM),LEE, HS (LEE, HYE SOOK)
- 학술지명 BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- 발행처명 KOREAN CHEMICAL SOC
- 발행국가 국내
- 논문언어 한국어
홈페이지논문 초록 (Abstract)
In the previous paper (Bull. Korean Chem. Soc., 2011, 32, 2997), the hybrid molecules between α-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.