Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 25, Issue 12, Pages 2946-2955Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2017.02.048
Keywords
Alzheimer's disease; Curcumin derivatives; AChE inhibition; A beta(1)-42 self-aggregation
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By fusing donepezil and curcumin, a novel series of compounds were obtained as multitarget-directed ligands against Alzheimer's disease. Among them, compound 11b displayed potent acetylcholinesterase (AChE) inhibition (IC50 = 187 nM) and the highest BuChE/AChE selectivity (66.3). Compound lib also inhibited 45.3% A beta(1-42) self-aggregation at 20 mu M and displayed remarkable antioxidant effects. The metal-chelating property of compound lib was elucidated by determining the 1:1 stoichiometry for the 11b-Cu(II) complex. The excellent blood-brain barrier permeability of 11b also indicated the potential for the compound to penetrate the central nervous system. (C) 2017 Elsevier Ltd. All rights reserved.
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