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Privileged Pharmacophore of FDA Approved Drugs in Combination with Chalcone Framework: A New Hope for Alzheimer’s Treatment

Bijo Mathew

2020Combinatorial Chemistry & High Throughput Screening14 citationsDOI

Abstract

Multi-functional design of ligands emerged as a new drug design paradigm of Alzheimer's disease (AD). Given the complexity of AD, the molecules showing dual inhibition of monoamine oxidase (MAO) and acetylcholinesterase (AChE) with neuroprotective properties could prevent the progressive neural degeneration effectively. Numerous studies documented that chalcone is a privileged structural framework for the inhibition of both MAO and AChE. The recent studies suggested that the development of chalcone candidates endowed with pharmacophores of FDA approved drugs may become an active molecules in the field of current AD research. The current perspective described the recent updates of chalcone moiety linked with the pharmacophores of flurbiprofen and rivastigmine hybrids as selective ChE/MAO-B inhibitors for the prophylactic agents for AD.

Topics & Concepts

ChalconePharmacophoreRivastigminePharmacologyNeuroprotectionAcetylcholinesteraseMonoamine oxidaseMonoamine oxidase BMedicineChemistryNeuroscienceStereochemistryBiochemistryDiseaseDementiaPsychologyEnzymeDonepezilInternal medicineCholinesterase and Neurodegenerative DiseasesComputational Drug Discovery MethodsSynthesis and biological activity
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