Acetylcholinesterase Inhibitors for Alzheimer’s disease: Past, Present, and Potential Future

Abstract

Alzheimer’s Diseases (AD) is a neurodegenerative disorder characterized by progressive neuronal loss leading to cognitive decline. Although there is yet to be a cure nor a way to reverse the neuronal damage, there are current treatments to amend some of the cognitive symptoms associated with AD. Acetylcholinesterase inhibitors (AChEi) are the primary agents of choice and have had profound implications throughout the past decades. AChEi such as donepezil, rivastigmine, and galantamine mediates and increases cholinergic activities in the central nervous system (CNS), and have been shown to improve and preserve cognition in AD patients. Beyond the current drugs on the market, investigational discoveries continue to explore the potential of safer and more efficacious AChEi agents for the treatment of AD. There have been quite a few challenges, given the high failure rates. Yet, these very trials and studies have been a fundamental step towards better understanding the treatments of AD and have provided some insight on the potential to surpass what is currently available.

Strychnos alkaloids: total synthesis, characterization, DFT investigations, and molecular docking with AChE, BuChE, and HSA

“…Hepatotoxicity profile and dosage frequency are common limitations of tacrine [ 108 ]. The IC 50 values of Donepezil, Rivastigmine, and Galantamine, which were approved by the FDA in the following years, were determined as 11.6 nM, ∼4.3nM, and 410 nM, respectively [ 109 , 110 , 111 ]. Molecular docking methods have also been frequently used for the detailed analysis of the interaction mechanisms of these drugs with various biomacromolecules.…”