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http://dx.doi.org/10.5012/jkcs.2016.60.2.125

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

Park, Jung-Youl (Industry-Academic Cooperation Foundation, Hanbat National University)
Shin, Sujeong (Department of Chemical & Biological Engineering, Hanbat National University)
Park, Kyoung Chan (Department of Chemical & Biological Engineering, Hanbat National University)
Jeong, Eunju (Department of Chemical & Biological Engineering, Hanbat National University)
Park, Jeong Ho (Department of Chemical & Biological Engineering, Hanbat National University)
Publication Information
Journal of the Korean Chemical Society / v.60, no.2, 2016 , pp. 125-130 More about this Journal
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.
Keywords
Triazole linked decursinol derivatives; Alzheimer’ s disease (AD); Acetylcholinesterase (AChE); Butyrylcholinesterase (BuChE);
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