Abstract
Due to the multifaceted pharmacological activities of chalcones, these scaffolds have been considered one of the most privileged frameworks in the drug discovery process. Structurally, chalcones are α, β-unsaturated carbonyl functionalities with two aryl or heteroaryl units. Amongst the numerous pharmacological activities explored for chalcone derivatives, the development of novel chalcone analogs for the treatment of Alzheimer’s disease (AD) is among the research topics of most interest. Chalcones possess numerous advantages, such as smaller molecular size, opportunities for further structural modification thereby altering the physicochemical properties, cost-effectiveness, and convenient synthetic methodology. The present review highlights the recent evidence of chalcones as a privileged structure in AD drug development processes. Different classes of chalcone-derived analogs are summarized for the easy understanding of the previously reported analogs as well as the importance of certain functionalities in exhibiting cholinesterase inhibition. In this way, this review will shed light on the medicinal chemistry fraternity for the design and development of novel promising chalcone candidates for the treatment of AD.
Highlights
Accepted: 10 March 2022A family of cholinesterase (ChE) catalyzes the hydrolysis of the neurotransmitter acetylcholine (ACh) into acetic acid and choline
The results revealed that carbamate moieties containing aliphatic amine groups and cyclic amine contributed to the eqBChE-inhibitory activity, but the arylamine produced an adverse effect on eqBChE-inhibitory activity
Though numerous medications are available for the management of these conditions, these medications lack certain kinds of efficacy parameters
Summary
A family of cholinesterase (ChE) catalyzes the hydrolysis of the neurotransmitter acetylcholine (ACh) into acetic acid and choline. Donepezil binds to the PAS and delays the deposition of amyloid plaque Rivastigmine inhibits both AChE and BChE by binding at the ecstatic part of the active site. Irreversible AChEIs exert their effects through the non-reversible phosphorylation of esterases in the central nervous system These are substrate analogs to ACh, and like natural substrate, they enter the active site via covalently binding to the serine–OH group [20]. Despite the fact that these substituted chalcones have a variety of medicinal uses and characteristics, their recognition abilities have yet to be investigated Chalcone serves as both an optical active moiety and a recognition unit in chalcone derivatives, allowing them to selectively detect target analytes [37], mainly focusing on current improvements in employing chalcone as a favored scaffold in medicinal chemistry, with an emphasis on research related to AD therapy as ChEIs. 2. Initial discussions in the present reports mainly focus on the incorporation of various substituents to the chalcone aromatic rings
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