콘텐츠 본문
논문 해외 국제전문학술지(SCI급) SYNTHESIS OF SELECTIVE BUTYRYLCHOLINESTERASE INHIBITORS COUPLED BETWEEN ALPHA-LIPOIC ACID AND POLYPHENOLS BY USING 2-(PIPERAZIN-1-YL)ETHANOL LINKER
- 학술지 구분 국제전문학술지(SCI급)
- 게재년월 2013-04
- 저자명 박정호
- 학술지명 BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- 발행처명 KOREAN CHEMICAL SOC
- 발행국가 해외
- 논문언어 외국어
- 전체저자수 7
논문 초록 (Abstract)
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 (BuC hE) inhibition. In order to increase the binding affinity of the hybr id compounds to cholinesterase (ChE), the neutral 2-(2-aminoethoxy)e thanol (linker 1) was switched to the cationic 2-(piperazin-1-yl)ethanol linker (linker 2). The IC50 values of the linker-2 hybrid molecul es for BuChE inhibition were lower than those of linker-1 hybrid molecul es (except 9-2) and they also had the same great selectivity for BuC hE over AChE (> 800 fold) as linker-1 hybrid molecules. ALA-acetyl c affeic acid (10-2, ALA-AcCA) was shown as an effective inhibitor of BuCh E (IC50 = 0.44 +/- 0.24 mu M). A kinetic study using 7-2 showed tha t it is the same mixed type inhibition as 7-1. Its inhibition constant (Ki) to BuChE is 4.3 +/-0.09 mu M.
