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

Five novel tacrine-ferulic acid hybrid compounds (8a–e) 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) aggregat...

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Autores principales: Fu, Yingbo, Mu, Yu, Lei, Hui, Wang, Pu, Li, Xin, Leng, Qiao, Han, Li, Qu, Xiaodan, Wang, Zhanyou, Huang, Xueshi
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273353/
https://www.ncbi.nlm.nih.gov/pubmed/27727187
http://dx.doi.org/10.3390/molecules21101338
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author Fu, Yingbo
Mu, Yu
Lei, Hui
Wang, Pu
Li, Xin
Leng, Qiao
Han, Li
Qu, Xiaodan
Wang, Zhanyou
Huang, Xueshi
author_facet Fu, Yingbo
Mu, Yu
Lei, Hui
Wang, Pu
Li, Xin
Leng, Qiao
Han, Li
Qu, Xiaodan
Wang, Zhanyou
Huang, Xueshi
author_sort Fu, Yingbo
collection PubMed
description Five novel tacrine-ferulic acid hybrid compounds (8a–e) 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 Cu(2+) 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 Cu(2+) and activity against Aβ-induced neurotoxicity in Neuro-2A cells.
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spelling pubmed-62733532018-12-28 Design, Synthesis and Evaluation of Novel Tacrine-Ferulic Acid Hybrids as Multifunctional Drug Candidates against Alzheimer’s Disease Fu, Yingbo Mu, Yu Lei, Hui Wang, Pu Li, Xin Leng, Qiao Han, Li Qu, Xiaodan Wang, Zhanyou Huang, Xueshi Molecules Article Five novel tacrine-ferulic acid hybrid compounds (8a–e) 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 Cu(2+) 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 Cu(2+) and activity against Aβ-induced neurotoxicity in Neuro-2A cells. MDPI 2016-10-11 /pmc/articles/PMC6273353/ /pubmed/27727187 http://dx.doi.org/10.3390/molecules21101338 Text en © 2016 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Fu, Yingbo
Mu, Yu
Lei, Hui
Wang, Pu
Li, Xin
Leng, Qiao
Han, Li
Qu, Xiaodan
Wang, Zhanyou
Huang, Xueshi
Design, Synthesis and Evaluation of Novel Tacrine-Ferulic Acid Hybrids as Multifunctional Drug Candidates against Alzheimer’s Disease
title Design, Synthesis and Evaluation of Novel Tacrine-Ferulic Acid Hybrids as Multifunctional Drug Candidates against Alzheimer’s Disease
title_full Design, Synthesis and Evaluation of Novel Tacrine-Ferulic Acid Hybrids as Multifunctional Drug Candidates against Alzheimer’s Disease
title_fullStr Design, Synthesis and Evaluation of Novel Tacrine-Ferulic Acid Hybrids as Multifunctional Drug Candidates against Alzheimer’s Disease
title_full_unstemmed Design, Synthesis and Evaluation of Novel Tacrine-Ferulic Acid Hybrids as Multifunctional Drug Candidates against Alzheimer’s Disease
title_short Design, Synthesis and Evaluation of Novel Tacrine-Ferulic Acid Hybrids as Multifunctional Drug Candidates against Alzheimer’s Disease
title_sort design, synthesis and evaluation of novel tacrine-ferulic acid hybrids as multifunctional drug candidates against alzheimer’s disease
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273353/
https://www.ncbi.nlm.nih.gov/pubmed/27727187
http://dx.doi.org/10.3390/molecules21101338
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