Abstract
The aim of this work is to review tacrine analogues from the last three years, which were not included in the latest review work, donepezil and galantamine hybrids from 2015 and rivastigmine derivatives from 2014. In this account, we summarize the efforts toward the development and characterization of non-toxic inhibitors of cholinesterases based on mentioned drugs with various interesting additional properties such as antioxidant, decreasing β-amyloid plaque aggregation, nitric oxide production, pro-inflammatory cytokines release, monoamine oxidase-B activity, cytotoxicity and oxidative stress in vitro and in animal model that classify these hybrids as potential multifunctional therapeutic agents for Alzheimer’s disease. Moreover, herein, we have described the cholinergic hypothesis, mechanisms of neurodegeneration and current pharmacotherapy of Alzheimer’s disease based on the restoration of cholinergic function through blocking enzymes that break down acetylcholine.
Keywords: Tacrine, donepezil, galantamine, rivastigmine, multifunctional cholinesterase inhibitors, alzheimer's disease.
Graphical Abstract
Current Neuropharmacology
Title:Therapeutic Potential of Multifunctional Derivatives of Cholinesterase Inhibitors
Volume: 19 Issue: 8
Author(s): Maja Przybyłowska, Krystyna Dzierzbicka, Szymon Kowalski, Klaudia Chmielewska and Iwona Inkielewicz-Stepniak*
Affiliation:
- Department of Pharmaceutical Pathophysiology, Faculty of Pharmacy, Medical University of Gdansk, Gdansk,Poland
Keywords: Tacrine, donepezil, galantamine, rivastigmine, multifunctional cholinesterase inhibitors, alzheimer's disease.
Abstract: The aim of this work is to review tacrine analogues from the last three years, which were not included in the latest review work, donepezil and galantamine hybrids from 2015 and rivastigmine derivatives from 2014. In this account, we summarize the efforts toward the development and characterization of non-toxic inhibitors of cholinesterases based on mentioned drugs with various interesting additional properties such as antioxidant, decreasing β-amyloid plaque aggregation, nitric oxide production, pro-inflammatory cytokines release, monoamine oxidase-B activity, cytotoxicity and oxidative stress in vitro and in animal model that classify these hybrids as potential multifunctional therapeutic agents for Alzheimer’s disease. Moreover, herein, we have described the cholinergic hypothesis, mechanisms of neurodegeneration and current pharmacotherapy of Alzheimer’s disease based on the restoration of cholinergic function through blocking enzymes that break down acetylcholine.
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Przybyłowska Maja , Dzierzbicka Krystyna , Kowalski Szymon , Chmielewska Klaudia and Inkielewicz-Stepniak Iwona *, Therapeutic Potential of Multifunctional Derivatives of Cholinesterase Inhibitors, Current Neuropharmacology 2021; 19 (8) . https://dx.doi.org/10.2174/1570159X19666201218103434
DOI https://dx.doi.org/10.2174/1570159X19666201218103434 |
Print ISSN 1570-159X |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6190 |
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