期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 20, 期 24, 页码 7214-7222出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.08.052
关键词
Coumarin; Benzylpyridinium; Actylcholinesterase inhibitor; Ellman's method
资金
- Research Council of Tehran University of Medical Sciences
- INSF (Iran National Science Foundation)
- National Institutes of Health (National Center for Research Resources) [2P41RR001081]
- National Institutes of Health (National Institute of General Medical Sciences) [9P41GM103311]
A novel series of coumarin derivatives linked to benzyl pyridinium group were synthesized and biologically evaluated as inhibitors of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The enzyme inhibitory activity of synthesized compounds was measured using colorimetric Ellman's method. It was revealed that compounds 3e, 3h, 3l, 3r and 3s have shown higher activity compared with donepezil hydrochloride as standard drug. Most of the compounds in these series had nanomolar range IC50 in which compound 3r (IC50 = 0.11 nM) was the most active compound against acetylcholinesterase enzyme. (C) 2012 Elsevier Ltd. All rights reserved.
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