ArticleScientific reports2019
Phenoxyethyl Piperidine/Morpholine Derivatives as PAS and CAS Inhibitors of Cholinesterases: Insights for Future Drug Design.
Article in Scientific reports, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 93 citations in OpenAlex.
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- New benzimidazole-alkanesulfonate conjugates as cholinesterase inhibitors with in vitro and in silico validation.Scientific reports · 2026Article
- Boron Containing Curcumin-Like Compound as an Acetylcholinesterase Inhibitor and Anticancer Agent: Synthesis, Biological Evaluation, and Computational Insights.Cell biochemistry and biophysics · 2026Article
- Dual Inhibitors of Acetylcholinesterase and Monoamine Oxidase-B for the Treatment of Alzheimer's Disease.Molecules (Basel, Switzerland) · 2025Review
- Therapeutic potential of morpholine-based compounds in neurodegenerative diseases: SAR insights and analysis.Future medicinal chemistry · 2025Review
- Determination of Acetylcholinesterase Activity Based on Ratiometric Fluorescence Signal Sensing.Journal of fluorescence · 2025Article
- Synthesis, Characterization, and Biological Effects of Chloro-Cathinones: Toxicity and Potential Neurological Impact.International journal of molecular sciences · 2025Article
- Contilisant-Belinostat Hybrids: Polyfunctionalized Indole Derivatives as Multineurotarget Drugs for the Potential Treatment of Alzheimer's Disease.ACS pharmacology & translational science · 2025Article
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- Synthesis, docking, pharmacokinetic prediction, and acetylcholinesterase inhibitory evaluation ofResearch in pharmaceutical sciences · 2024Article
- Assessing the Potential of 1,2,3-Triazole-Dihydropyrimidinone Hybrids Against Cholinesterases: In Silico, In Vitro, and In Vivo Studies.International journal of molecular sciences · 2024Article
- Evaluation of forces applied to tissues during robotic-assisted surgical tasks using a novel force feedback technology.Surgical endoscopy · 2024Article
- Design of Promising Thiazoloindazole-Based Acetylcholinesterase Inhibitors Guided by Molecular Docking and Experimental Insights.ACS chemical neuroscience · 2024Article
- Ceanothanes Derivatives as Peripheric Anionic Site and Catalytic Active Site Inhibitors of Acetylcholinesterase: Insights for Future Drug Design.International journal of molecular sciences · 2024Article
- Article
- Design of electron-donating group substituted 2-PAM analogs as antidotes for organophosphate insecticide poisoning.RSC advances · 2023Article
- Investigation on NovelMolecules (Basel, Switzerland) · 2023Article
- Validation of Acetylcholinesterase Inhibition Machine Learning Models for Multiple Species.Chemical research in toxicology · 2023Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Acetylcholinesterase (AChE) catalyzes the conversion of Aβ peptide to its aggregated form and the peripheral anionic site (PAS) of AChE is mainly involved in this phenomenon. Also catalytic active site (CAS) of donepezil stimulates the break-down of acetylcholine (ACh) and depletion of ACh in cholinergic synapses are well established in brains of patients with AD. In this study, a set of compounds bearing phenoxyethyl amines were synthesized and their inhibitory activity toward electric eel AChE (eeAChE) and equine butyrylcholinesterase (eqBuChE) were evaluated. Molecular dynamics (MD) was employed to record the binding interactions of best compounds against human cholinesterases (hAChE and hBuChE) as well as donepezil as reference drug. In vitro results revealed that compound 5c is capable of inhibiting eeAChE activity at IC
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