ArticleScientific reports2016
Development of an in-vivo active reversible butyrylcholinesterase inhibitor.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 54 papers.
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Who cites it
54 citing papers in PubMed, 159 citations in OpenAlex.
- Dual Inhibitors of p38α Mitogen-Activated Protein Kinase and Butyrylcholinesterase for the Modulation of Neuroinflammation and Cognitive Dysfunction.Journal of medicinal chemistry · 2026Article
- Molecular Mechanistic Studies on Caffeoylquinic Acid Derivatives From Vaccinium dunalianum Wight as Dual-Target Inhibitors of AChE and BChE With In Vitro Inhibitory Evaluation and Molecular Docking.Chemistry & biodiversity · 2026Article
- Structural engineering, BSA binding and computational analysis of isonipacotate based enzyme inhibitors containing 1,2,4-triazole.PloS one · 2026Article
- Development of Novel 3‑Phenylpropanamide Derivatives as BChE Inhibitors for the Treatment of Alzheimer's Disease.ACS omega · 2025Article
- Targeting Neuroinflammation and Cognitive Decline: First-in-Class Dual Butyrylcholinesterase and p38α Mitogen-Activated Protein Kinase Inhibitors.Journal of medicinal chemistry · 2025Article
- Pharmacological Evaluation of a Traditional Thai Polyherbal Formula for Alzheimer's Disease: Evidence from In Vitro and In Silico Studies.International journal of molecular sciences · 2025Article
- Lead Optimization of a Butyrylcholinesterase Inhibitor for the Treatment of Alzheimer's Disease.Journal of medicinal chemistry · 2025Article
- Discovery, Biological Evaluation and Binding Mode Investigation of Novel Butyrylcholinesterase Inhibitors Through Hybrid Virtual Screening.Molecules (Basel, Switzerland) · 2025Article
- Chromatographic Analysis and Enzyme Inhibition Potential ofPharmaceuticals (Basel, Switzerland) · 2025Article
- Design of New Aromatic Tertiary Amine-based as Butyrylcholinesterase Inhibitors Relying on Molecular Docking, ADME-Tox and Molecular Dynamics.Current computer-aided drug design · 2025Article
- Novel anti-neuroinflammatory pyranone-carbamate derivatives as selective butyrylcholinesterase inhibitors for treating Alzheimer's disease.Journal of enzyme inhibition and medicinal chemistry · 2024Article
- The selective butyrylcholinesterase inhibitor UW-MD-95 shows symptomatic and neuroprotective effects in a pharmacological mouse model of Alzheimer's disease.CNS neuroscience & therapeutics · 2024Article
- Innovation of 6-sulfonamide-2RSC advances · 2024Article
- Indole-Based Compounds in the Development of Anti-Neurodegenerative Agents.Molecules (Basel, Switzerland) · 2024Review
- Exploration of a library of piperonylic acid-derived hydrazones possessing variable aryl functionalities as potent dual cholinesterase and monoamine oxidase inhibitors.Molecular diversity · 2023Article
- The Antioxidant and Neuroprotective Potential of Leaves and Inflorescences Extracts of Selected Hemp Varieties Obtained with scCOAntioxidants (Basel, Switzerland) · 2023Article
- 8-Hydroxyquinolylnitrones as multifunctional ligands for the therapy of neurodegenerative diseases.Acta pharmaceutica Sinica. B · 2023Article
- Exploiting butyrylcholinesterase inhibitors through a combined 3-D pharmacophore modeling, QSAR, molecular docking, and molecular dynamics investigation.RSC advances · 2023Article
- In silico and in vitro studies confirm Ondansetron as a novel acetylcholinesterase and butyrylcholinesterase inhibitor.Scientific reports · 2023Article
- Potential revival of cholinesterase inhibitors as drugs in veterinary medicine.Frontiers in veterinary science · 2023Review
Corrections and comments
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Authors and funding
25 authors at 4 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Alzheimer's disease (AD) is characterized by severe basal forebrain cholinergic deficit, which results in progressive and chronic deterioration of memory and cognitive functions. Similar to acetylcholinesterase, butyrylcholinesterase (BChE) contributes to the termination of cholinergic neurotransmission. Its enzymatic activity increases with the disease progression, thus classifying BChE as a viable therapeutic target in advanced AD. Potent, selective and reversible human BChE inhibitors were developed. The solved crystal structure of human BChE in complex with the most potent inhibitor reveals its binding mode and provides the molecular basis of its low nanomolar potency. Additionally, this compound is noncytotoxic and has neuroprotective properties. Furthermore, this inhibitor moderately crosses the blood-brain barrier and improves memory, cognitive functions and learning abilities of mice in a model of the cholinergic deficit that characterizes AD, without producing acute cholinergic adverse effects. Our study provides an advanced lead compound for developing drugs for alleviating symptoms caused by cholinergic hypofunction in advanced AD.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.