122nd General Meeting of the KCS

Type Poster Presentation
Area Medicinal Chemistry
Room No. Grand Ballroom
Time 10월 18일 (목요일) 11:00~12:30
Code MEDI.P-288
Subject Synthesis of Paeonol Derivatives and their Cholinesterase Inhibitory Activity toward Development of Alzheimer's Drug Candidates
Authors Cheolmin Jeon, Yujung Kang*, Haneul Lee, Jeong Ho Park1,*
Department of Chemical & Biological Engineering, Hanbat National University, Korea
1Division of Applied Chemistry & Biological Enginee, Hanbat National University, Korea
Abstract Alzheimer’s disease (AD) is the most common neurodegenerative disease among the cause of dementia which can appear in the elderly people aged 65 or old. The cause of Alzheimer's disease is not yet known exactly. Alzheimer's drugs based on the cholinergic theory currently marketed for the treatment of AD patient. However, they have some side effects. We have been researching to find out new candidate compounds as cholinesterase inhibitors. In this study, a series of paeonol compounds were synthesized and their in vitro cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibitory activities were evaluated. The structure-activity relationship (SAR) study depended on the Claig plot was carried out ; plotting the sigma constants of the Hammett equation (σ) versus hydrophobicity (π). The IC50 value of compound 5 (+σ, +π) is 0.26 ± 0.06 μM and it is comparable to that of galantamine (IC50 = 12.74 ± 0.86μM against BuChE).
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