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Molecules 2016, 21(10), 1338; doi:10.3390/molecules21101338

Design, Synthesis and Evaluation of Novel Tacrine-Ferulic Acid Hybrids as Multifunctional Drug Candidates against Alzheimer’s Disease

1
Laboratory of Metabolic Disease Research and Drug Development, China Medical University, Shenyang 110001, China
2
Institute of Microbial Pharmaceuticals, College of Life and Health Sciences, Northeastern University, Shenyang 110819, China
*
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 2 August 2016 / Revised: 4 October 2016 / Accepted: 7 October 2016 / Published: 11 October 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [1531 KB, uploaded 11 October 2016]   |  

Abstract

Five novel tacrine-ferulic acid hybrid compounds (8ae) were synthesized and their structures were identified on the basis of a detailed spectroscopic analysis. The activities of inhibiting acetyl cholinesterase (AChE) and butyryl cholinesterase (BuChE), reducing self-induced β-amyloid (Aβ) aggregation and chelating Cu2+ were evaluated in vitro. Among them, 8c and 8d displayed the higher selectivity in inhibiting AChE over BuChE. Moreover, 8d also showed dramatic inhibition of self-Aβ aggregation, activity of chelating Cu2+ and activity against Aβ-induced neurotoxicity in Neuro-2A cells. View Full-Text
Keywords: β-amyloid aggregation; cholinesterase; ferulic acid; metal chelator; tacrine; neuroprotection β-amyloid aggregation; cholinesterase; ferulic acid; metal chelator; tacrine; neuroprotection
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Fu, Y.; Mu, Y.; Lei, H.; Wang, P.; Li, X.; Leng, Q.; Han, L.; Qu, X.; Wang, Z.; Huang, X. Design, Synthesis and Evaluation of Novel Tacrine-Ferulic Acid Hybrids as Multifunctional Drug Candidates against Alzheimer’s Disease. Molecules 2016, 21, 1338.

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