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Inhibitory potential of nitrogen, oxygen and sulfur containing heterocyclic scaffolds against acetylcholinesterase and butyrylcholinesterase

Rami J. Obaid, Nafeesa Naeem, Ehsan Ullah Mughal, Munirah M. Al‐Rooqi, Amina Sadiq, Rabab S. Jassas, Ziad Moussa, Saleh A. Ahmed

2022RSC Advances128 citationsDOIOpen Access PDF

Abstract

Most frequently, pure nitrogen heterocycles or various positional combinations of nitrogen, oxygen, and sulfur atoms in five or six-membered rings can be found. Inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes is a popular strategy for the management of numerous mental diseases. In this context, cholinesterase inhibitors are utilized to relieve the symptoms of neurological illnesses like dementia and Alzheimer's disease (AD). The present review focuses on various heterocyclic scaffolds and their role in designing and developing new potential AChE and BChE inhibitors to treat AD. Moreover, a detailed structure-activity relationship (SAR) has been established for the future discovery of novel drugs for the treatment of AD. Most of the heterocyclic motifs have been used in the design of new potent cholinesterase inhibitors. In this regard, this review is an endeavor to summarize the biological and chemical studies over the past decade (2010-2022) describing the pursuit of new N, O and S containing heterocycles which can offer a rich supply of promising AChE and BChE inhibitory activities.

Topics & Concepts

ButyrylcholinesteraseAcetylcholinesteraseCholinesteraseChemistryContext (archaeology)Combinatorial chemistryAchéPharmacologyEnzymeOrganic chemistryMedicineBiologyPaleontologyCholinesterase and Neurodegenerative DiseasesComputational Drug Discovery MethodsSynthesis and biological activity
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