{"title":"Recent Advances in The Therapeutic Insights of Thiazole Scaffolds as Acetylcholinesterase Inhibitors","authors":"Dina H. Dawood, Manal M. Anwar","doi":"10.1016/j.ejmech.2025.117331","DOIUrl":null,"url":null,"abstract":"Suppression of the acetylcholinesterase (AChE) enzyme is a prevalent strategy for curing diverse mental disorders, including Alzheimer’s disease (AD) and the chronic autoimmune disease Myasthenia gravis. Acetylcholinesterase inhibitors promote cholinergic transmission via blocking AChE, which is implicated in the degradation and deficiency of acetylcholine. Various studies proved that the lack of cholinergic neurons in the central nervous system is the substantial reason for the behavioral abnormalities and cognitive retogradation that distinguish mental diseases such as dementia and AD. Moreover, thiazole scaffolds have emerged as prominent pharmacophores in drug discovery owing to their numerous outstanding therapeutic efficacy, comprising anti-acetylcholinesterase efficacy. This review presents various thiazole-based AChE inhibitors in the recent decade. In addition, the various interactions of thiazole derivatives within the active pocket of AChE have been highlighted.","PeriodicalId":314,"journal":{"name":"European Journal of Medicinal Chemistry","volume":"60 1","pages":""},"PeriodicalIF":6.0000,"publicationDate":"2025-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"European Journal of Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1016/j.ejmech.2025.117331","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
Suppression of the acetylcholinesterase (AChE) enzyme is a prevalent strategy for curing diverse mental disorders, including Alzheimer’s disease (AD) and the chronic autoimmune disease Myasthenia gravis. Acetylcholinesterase inhibitors promote cholinergic transmission via blocking AChE, which is implicated in the degradation and deficiency of acetylcholine. Various studies proved that the lack of cholinergic neurons in the central nervous system is the substantial reason for the behavioral abnormalities and cognitive retogradation that distinguish mental diseases such as dementia and AD. Moreover, thiazole scaffolds have emerged as prominent pharmacophores in drug discovery owing to their numerous outstanding therapeutic efficacy, comprising anti-acetylcholinesterase efficacy. This review presents various thiazole-based AChE inhibitors in the recent decade. In addition, the various interactions of thiazole derivatives within the active pocket of AChE have been highlighted.
期刊介绍:
The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers.
A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.