Jia Wang
Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II)
Wang, Jia; Wang, Chaolei; Wu, Zheng; Li, Xinnan; Xu, Shengtao; Liu, Jie; Lan, Qinying; Zhu, Zheying; Xu, Jinyi
Authors
Chaolei Wang
Zheng Wu
Xinnan Li
Shengtao Xu
Jie Liu
Qinying Lan
ZHEYING ZHU Zheying.Zhu@nottingham.ac.uk
Associate Professor in International Pharmacy and Traditional Medicines
Jinyi Xu
Abstract
A series of novel 4-isochromanone compounds bearing N-benzyl pyridinium moiety were designed and synthesized as acetylcholinesterase (AChE) inhibitors. The biological evaluation showed that most of the target compounds exhibited potent inhibitory activities against AChE. Among them, compound 1q possessed the strongest anti-AChE activity with an IC50 value of 0.15 nM and high AChE/BuChE selectivity (SI >5000). Moreover, compound 1q had low toxicity in normal nerve cells and was relatively stable in rat plasma. Together, the current finding may provide a new approach for the discovery of novel anti-Alzheimer’s disease agents.
Citation
Wang, J., Wang, C., Wu, Z., Li, X., Xu, S., Liu, J., …Xu, J. (2018). Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II). Chemical Biology and Drug Design, 91(3), 756-762. https://doi.org/10.1111/cbdd.13136
Journal Article Type | Article |
---|---|
Acceptance Date | Oct 14, 2017 |
Online Publication Date | Nov 7, 2017 |
Publication Date | Feb 21, 2018 |
Deposit Date | Oct 26, 2017 |
Publicly Available Date | Nov 8, 2018 |
Journal | Chemical Biology and Drug Design |
Print ISSN | 1747-0277 |
Electronic ISSN | 1747-0285 |
Publisher | Wiley |
Peer Reviewed | Peer Reviewed |
Volume | 91 |
Issue | 3 |
Pages | 756-762 |
DOI | https://doi.org/10.1111/cbdd.13136 |
Keywords | Alzheimer’s disease, acetylcholinesterase inhibitors, 4-isochromanone skeleton, benzyl pyridine |
Public URL | https://nottingham-repository.worktribe.com/output/913293 |
Publisher URL | http://onlinelibrary.wiley.com/doi/10.1111/cbdd.13136/abstract |
Additional Information | This is the pre-peer reviewed version of the following article: Wang J, Wang C, Wu Z, et al. Design, synthesis, biological evaluation, and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II). Chem Biol Drug Des. 2018;91:756–762, which has been published in final form at http://onlinelibrary.wiley.com/doi/10.1111/cbdd.13136/abstract. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Self-Archiving. |
Contract Date | Oct 26, 2017 |
Files
CBDD 2017-accepted.pdf
(990 Kb)
PDF
You might also like
The structural modification of natural products for novel drug discovery
(2016)
Journal Article
Downloadable Citations
About Repository@Nottingham
Administrator e-mail: discovery-access-systems@nottingham.ac.uk
This application uses the following open-source libraries:
SheetJS Community Edition
Apache License Version 2.0 (http://www.apache.org/licenses/)
PDF.js
Apache License Version 2.0 (http://www.apache.org/licenses/)
Font Awesome
SIL OFL 1.1 (http://scripts.sil.org/OFL)
MIT License (http://opensource.org/licenses/mit-license.html)
CC BY 3.0 ( http://creativecommons.org/licenses/by/3.0/)
Powered by Worktribe © 2024
Advanced Search