ArticleMolecules (Basel, Switzerland)2016
Novel Triazole-Quinoline Derivatives as Selective Dual Binding Site Acetylcholinesterase Inhibitors.
Article in Molecules (Basel, Switzerland), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 59 citations in OpenAlex.
- Design, Synthesis, In Vitro and In Vivo Evaluation of Novel Anti-Alzheimer's (1Pharmaceuticals (Basel, Switzerland) · 2026Article
- Quinoline/thiazole compounds as selective acetylcholinesterase inhibitors: synthesis and biological assessment.RSC 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
- Multifunctional Tacrine-Quinoline Hybrids as Cholinesterase Inhibitors, Aβ Aggregation Blockers, and Metal Chelators for Alzheimer's Therapy.Molecules (Basel, Switzerland) · 2025Article
- Pentacyclic aromatic heterocycles from Pd-catalyzed annulation of 1,5-diaryl-1,2,3-triazoles.Beilstein journal of organic chemistry · 2025Article
- Diagnostic implications of ubiquitination-related gene signatures in Alzheimer's disease.Scientific reports · 2024Article
- Review
- Application of Quinoline Ring in Structural Modification of Natural Products.Molecules (Basel, Switzerland) · 2023Review
- An Overview of 1,2,3-triazole-Containing Hybrids and Their Potential Anticholinesterase Activities.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Inhibitory potential of nitrogen, oxygen and sulfur containing heterocyclic scaffolds against acetylcholinesterase and butyrylcholinesterase.RSC advances · 2022Review
- Antimicrobial Activity of Quinoline-Based Hydroxyimidazolium Hybrids.Antibiotics (Basel, Switzerland) · 2019Article
- Synthesis and Properties of 6-Aryl-4-azidocinnolines and 6-Aryl-4-(1,2,3-1Molecules (Basel, Switzerland) · 2019Article
- Synthesis and Inhibition Evaluation of New Benzyltetrahydroprotoberberine Alkaloids Designed as Acetylcholinesterase Inhibitors.Frontiers in chemistry · 2019Article
- In silico repurposing of antipsychotic drugs for Alzheimer's disease.BMC neuroscience · 2017Article
- Special Issue: "Molecules against Alzheimer".Molecules (Basel, Switzerland) · 2016Article
- Crystal structures of 6-chloro-indan-1-one and 6-bromo-indan-1-one exhibit different inter-molecular packing inter-actions.Acta crystallographica. Section E, Crystallographic communications · 2016Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Alzheimer's disease (AD) is the most prevalent neurodegenerative disorder worldwide. Currently, the only strategy for palliative treatment of AD is to inhibit acetylcholinesterase (AChE) in order to increase the concentration of acetylcholine in the synaptic cleft. Evidence indicates that AChE also interacts with the β-amyloid (Aβ) protein, acting as a chaperone and increasing the number and neurotoxicity of Aβ fibrils. It is known that AChE has two binding sites: the peripheral site, responsible for the interactions with Aβ, and the catalytic site, related with acetylcholine hydrolysis. In this work, we reported the synthesis and biological evaluation of a library of new tacrine-donepezil hybrids, as a potential dual binding site AChE inhibitor, containing a triazole-quinoline system. The synthesis of hybrids was performed in four steps using the click chemistry strategy. These compounds were evaluated as hAChE and hBChE inhibitors, and some derivatives showed IC50 values in the micro-molar range and were remarkably selective towards hAChE. Kinetic assays and molecular modeling studies confirm that these compounds block both catalytic and peripheral AChE sites. These results are quite interesting since the triazole-quinoline system is a new structural scaffold for AChE inhibitors. Furthermore, the synthetic approach is very efficient for the preparation of target compounds, allowing a further fruitful new chemical library optimization.
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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.