Enzyme‐Mediated In Situ Self‐Assembly AIE Probes: Mapping the Distribution of Acetylcholinesterase in Aging Mice Brain
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DOI: 10.1002/adfm.202425074
Abstract: Acetylcholinesterase (AChE) exhibits profound association with the underlying pathological mechanisms of aging‐related disorders. However, revealing the spatial distribution of AChE among whole‐brain remains an uncharted territory, posing a substantial challenge. Herein, a dual regulation strategy… read more here.
Keywords: brain; distribution; acetylcholinesterase; ache ... See more keywords
Synthesis, biological evaluation, and docking studies of some 5‐chloro‐2(3H)‐benzoxazolone Mannich bases derivatives as cholinesterase inhibitors
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DOI: 10.1002/ardp.201700273
Abstract: A series of N‐substituted‐5‐chloro‐2(3H)‐benzoxazolone derivatives were synthesized and evaluated for their acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) inhibitory, and antioxidant activities. The structures of the title compounds were confirmed by spectral and elemental analyses. The cholinesterase (ChE)… read more here.
Keywords: ache; chloro benzoxazolone; compound; synthesis biological ... See more keywords
Toward the cholinesterase inhibition potential of TADDOL derivatives: Seminal biological and computational studies
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DOI: 10.1002/ardp.202200142
Abstract: Alzheimer's disease (AD) is a degenerative neurological disease characterized by gradual loss of cognitive skills and memory. The exact pathogenesis involved still remains unrevealed, but several studies indicate the involvement of an array of different… read more here.
Keywords: inhibition; toward cholinesterase; taddol derivatives; cholinesterase inhibition ... See more keywords
New benzimidazole–indole–amide derivatives as potent α‐glucosidase and acetylcholinesterase inhibitors
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DOI: 10.1002/ardp.202400354
Abstract: New derivatives 6a–m with benzimidazole–indole–amide scaffold were developed, synthesized, and assessed for potential inhibitory effects on α‐glucosidase and acetylcholinesterase (AChE). These compounds were synthesized by various amine derivatives. With the exception of two compounds, the… read more here.
Keywords: benzimidazole indole; indole amide; glucosidase acetylcholinesterase; ache ... See more keywords
Dual Inhibition of AChE and GST by 1,2,4-Triazine-3-Amine: Integrated Biochemical, Computational, and Hepatotoxicity Insights.
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DOI: 10.1002/bab.70098
Abstract: 1,2,4-Triazine-3-amines (TzAs) are a group of compounds having a triazine ring and generally have a heterocyclic structure containing three nitrogen atoms. Studies have revealed that these compounds may exhibit antitumor, antimicrobial, anti-inflammatory, and antiviral properties.… read more here.
Keywords: dual inhibition; gst; triazine; ache ... See more keywords
Novel Pyridine‐Containing Sultones: Structure‐Activity Relationship and Biological Evaluation as Selective AChE Inhibitors for the Treatment of Alzheimer's disease
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DOI: 10.1002/cmdc.202100272
Abstract: Novel pyridine‐containing sultones were synthesized and evaluated for their cholinesterase (ChE) inhibitory activity. Most of compounds showed selective acetylcholinesterase (AChE) inhibitory activity. The structure‐activity relationship (SAR) showed: (i) the fused pyridine‐containing sultones increase AChE inhibition,… read more here.
Keywords: ache; novel pyridine; containing sultones; pyridine containing ... See more keywords
Design, synthesis, and structure–activity relationship of caffeine‐based triazoles as dual AChE and BACE‐1 inhibitors
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DOI: 10.1002/ddr.21998
Abstract: Natural products have significantly contributed to drug discovery for neurodegenerative diseases. Caffeine is one of the well‐known central nervous system(CNS)‐active natural products. Besides its CNS stimulant properties, it is a mild inhibitor of acetylcholinesterase (AChE)… read more here.
Keywords: bace; caffeine based; caffeine; ache ... See more keywords
Screening Natural Phenolic Compounds for Blood-Brain Barrier Permeability, Alongside GSK-3β, CK-1δ, and AChE Inhibition, for the Treatment of Alzheimer's Disease.
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DOI: 10.1002/ddr.70193
Abstract: Alzheimer's Disease (AD) is a neurological disorder characterized by progressive cognitive impairment and memory loss. In vitro artificial membrane permeability assays targeting the blood‐brain barrier (BBB), such as the parallel artificial membrane permeability assay (PAMPA),… read more here.
Keywords: alzheimer disease; disease; permeability; ache ... See more keywords
Covalent immobilization of acetylcholinesterase on a novel polyacrylic acid‐based nanofiber membrane
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DOI: 10.1002/elsc.201700130
Abstract: In this study, polyacrylic acid‐based nanofiber (NF) membrane was prepared via electrospinning method. Acetylcholinesterase (AChE) from Electrophorus electricus was covalently immobilized onto polyacrylic acid‐based NF membrane by demonstrating efficient enzyme immobilization, and immobilization capacity of… read more here.
Keywords: ache; acid based; immobilization; polyacrylic acid ... See more keywords
Reactivation by novel pyridinium oximes of rat serum and skeletal muscle acetylcholinesterase inhibited by organophosphates
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DOI: 10.1002/jbt.23750
Abstract: The treatment of organophosphate (OP) anticholinesterases currently lacks an effective oxime reactivator of OP‐inhibited acetylcholinesterase (AChE) which can penetrate the blood‐brain barrier (BBB). Our laboratories have synthesized novel substituted phenoxyalkyl pyridinium oximes and tested them… read more here.
Keywords: skeletal muscle; pyridinium oximes; reactivation; ache ... See more keywords
In silico analyses of acetylcholinesterase (AChE) and its genetic variants in interaction with the anti‐Alzheimer drug Rivastigmine
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Cellular Biochemistry"
DOI: 10.1002/jcb.30277
Abstract: Alzheimer's disease (AD) is the leading cause of dementia worldwide. Despite causing great social and economic impact, there is currently no cure for AD. The most effective therapy to manage AD symptoms is based on… read more here.
Keywords: analyses acetylcholinesterase; interaction; ache; silico analyses ... See more keywords