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Synthesis and in vitro Assay of New Triazole Linked Decursinol Derivatives Showing Inhibitory Activity against Cholinesterase for Alzheimer’s Disease Therapeutics

대한화학회지 2016년 60권 2호 p.125 ~ 130
 ( Park Jung-Youl ) - Hanbat National University Industry-Academic Cooperation Foundation

 ( Shin Su-Jeong ) - Hanbat National University Department of Chemical and Biological Engineering
 ( Park Kyoung-Chan ) - Hanbat National University Department of Chemical and Biological Engineering
 ( Jeong Eun-Ju ) - Hanbat National University Department of Chemical and Biological Engineering
 ( Park Jeong-Ho ) - Hanbat National University Department of Chemical and Biological Engineering

Abstract


With the goal of developing Alzheimer’s disease therapeutics, we have designed and synthesized new triazole linked decursinol derivatives having potency inhibitory activities against cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)]. Since inhibition of cholinesterase (ChE) is still considered to be one of the most effective targets to treat AD patients, many new classes of ChE inhibitors have been synthesized. In an effort of identifying new type of cholinergic drug, decursinol derivatives 11-17 have been synthesized between decursinol and other biological interesting compounds such as lipoic acid, polyphenols, etc by using the click reaction and then evaluated their biological activities. Compound 12 (IC50 = 5.89 ± 0.31 mM against BuChE) showed more effective inhibitory activity against BuChE than galantamine (IC50 = 9.4 ± 2.5 mM). Decursinol derivatives can be considered a new class inhibitor for BuChE and can be applied to be a novel drug candidate to treat AD patients.

키워드

Triazole linked decursinol derivatives; Alzheimer’s disease (AD); Acetylcholinesterase (AChE); Butyrylcholinesterase(BuChE)
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