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Current Neuropharmacology

Editor-in-Chief

ISSN (Print): 1570-159X
ISSN (Online): 1875-6190

Review Article

Therapeutic Potential of Multifunctional Derivatives of Cholinesterase Inhibitors

Author(s): Maja Przybyłowska, Krystyna Dzierzbicka, Szymon Kowalski, Klaudia Chmielewska and Iwona Inkielewicz-Stepniak*

Volume 19, Issue 8, 2021

Published on: 17 December, 2020

Page: [1323 - 1344] Pages: 22

DOI: 10.2174/1570159X19666201218103434

Price: $65

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


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