[Pubmed] Recent advances in the therapeutic insights of thiazole scaffolds as acetylcholinesterase inhibitors

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Eur J Med Chem. 2025 Jan 30;287:117331. doi: 10.1016/j.ejmech.2025.117331. Online ahead of print.

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. Also, structure-activity relationship (SAR) has been discussed.

PMID:39938408 | DOI:10.1016/j.ejmech.2025.117331


Source: https://pubmed.ncbi.nlm.nih.gov/3993840 ... t9+e462414