Please use this identifier to cite or link to this item: http://hdl.handle.net/10397/8227
Title: Synthesis and pharmacological evaluation of multifunctional tacrine derivatives against several disease pathways of AD
Authors: Digiacomo, M
Chen, Z
Wang, S
Lapucci, A
Macchia, M
Yang, X
Chu, J
Han, Y 
Pi, R
Rapposelli, S
Keywords: Alzheimer's disease
Amyloid protein
BACE1
Caffeic acid
Copper
Multi-targeted ligands
Tacrine
Issue Date: 2015
Publisher: Pergamon Press
Source: Bioorganic & medicinal chemistry letters, 2015 How to cite?
Journal: Bioorganic & medicinal chemistry letters 
Abstract: A novel series of tacrine derivatives were designed and synthesized by combining caffeic acid (CA), ferulic acid (FA) and lipoic acid (LA) with tacrine. The antioxidant study revealed that all the hybrids have much more antioxidant capacities compared to CA. Among these compounds, 1b possessed a good ability to inhibit the β-amyloid protein (Aβ) self-aggregation, sub-micromole acetylcholinesterase (AChE)/butyrylcholinesterase (BuChE) inhibitory, modest BACE1 inhibitory. Moreover, compound 1b also was a DPPH radical scavenger and copper chelatory as well as had potent neuroprotective effects against glutamate-induced cell death with low toxicity in HT22 cells. Our findings suggest that the compound 1b might be a promising lead multi-targeted ligand and worthy of further developing for the therapy of Alzheimer's disease.
URI: http://hdl.handle.net/10397/8227
ISSN: 0960-894X
EISSN: 1464-3405
DOI: 10.1016/j.bmcl.2014.12.084
Appears in Collections:Journal/Magazine Article

Access
View full-text via PolyU eLinks SFX Query
Show full item record

SCOPUSTM   
Citations

19
Last Week
3
Last month
0
Citations as of Jan 8, 2018

WEB OF SCIENCETM
Citations

17
Last Week
0
Last month
0
Citations as of Jan 15, 2018

Page view(s)

57
Last Week
2
Last month
Citations as of Jan 14, 2018

Google ScholarTM

Check

Altmetric


Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.