ArticleJournal of enzyme inhibition and medicinal chemistry2020
Novel tacrine-benzofuran hybrids as potential multi-target drug candidates for the treatment of Alzheimer's Disease.
Article in Journal of enzyme inhibition and medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 65 citations in OpenAlex.
- Highly Efficient and Eco-friendly Synthesis and Bio-activities of 1,3-benzazoles as Cu (II) Chelators in Alzheimer's Disease Therapy.Current medicinal chemistry · 2026Article
- Phytomedicine Potential ofPlants (Basel, Switzerland) · 2025Article
- Computational Approaches for Multitarget Drug Design in Alzheimer's Disease: A Comprehensive Review.Current medicinal chemistry · 2025Review
- A Review on Phytochemical Constituents used as Current Treatment Strategies for Neurodegenerative Disease.Anti-inflammatory & anti-allergy agents in medicinal chemistry · 2025Review
- Targeting Neurodegeneration: The Emerging Role of Hybrid Drugs.Current drug targets · 2025Review
- Hybrid/Chimera Drugs - Part 1 - Drug Hybrids Affecting Diseases of the Central Nervous System.Current medicinal chemistry · 2025Review
- Recent advances in potential enzymes and their therapeutic inhibitors for the treatment of Alzheimer's disease.Heliyon · 2024Review
- Therapeutic Options in Alzheimer's Disease: From Classic Acetylcholinesterase Inhibitors to Multi-Target Drugs with Pleiotropic Activity.Life (Basel, Switzerland) · 2024Article
- Metabolites profiling, in-vitro and molecular docking studies of five legume seeds for Alzheimer's disease.Scientific reports · 2024Article
- Discovery of novel 1,2,4-triazole tethered β-hydroxy sulfides as bacterial tyrosinase inhibitors: synthesis and biophysical evaluation throughRSC advances · 2024Article
- Deciphering Neuroprotective Effect ofCurrent drug targets · 2024Review
- Unfolding the Antibacterial Activity and Acetylcholinesterase Inhibition Potential of Benzofuran-Triazole Hybrids: Synthesis, Antibacterial, Acetylcholinesterase Inhibition, and Molecular Docking Studies.Molecules (Basel, Switzerland) · 2023Article
- Discovery of Novel Coumarin-Schiff Base Hybrids as Potential Acetylcholinesterase Inhibitors: Design, Synthesis, Enzyme Inhibition, and Computational Studies.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Tacrine-Based Hybrids: Past, Present, and Future.International journal of molecular sciences · 2023Review
- Antioxidant Compounds in the Treatment of Alzheimer's Disease: Natural, Hybrid, and Synthetic Products.Evidence-based complementary and alternative medicine : eCAM · 2023Review
- Design, synthesis and biological evaluation of novelJournal of enzyme inhibition and medicinal chemistry · 2022Article
- Molecular Insights into Therapeutic Potentials of Hybrid Compounds Targeting Alzheimer's Disease.Molecular neurobiology · 2022Review
- Neuroprotective Effects of Cholinesterase Inhibitors: Current Scenario in Therapies for Alzheimer's Disease and Future Perspectives.Journal of Alzheimer's disease reports · 2022Review
- Acetylcholinesterase Inhibitors in the Treatment of Neurodegenerative Diseases and the Role of Acetylcholinesterase in their Pathogenesis.International journal of molecular sciences · 2021Review
- Derivatives of Tenuazonic Acid as Potential New Multi-Target Anti-Alzheimer's Disease Agents.Biomolecules · 2021Article
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Authors and funding
9 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Pursuing the widespread interest on multi-target drugs to combat Alzheimer´s disease (AD), a new series of hybrids was designed and developed based on the repositioning of the well-known acetylcholinesterase (AChE) inhibitor, tacrine (TAC), by its coupling to benzofuran (BF) derivatives. The BF framework aims to endow the conjugate molecules with ability for inhibition of AChE (bimodal way) and of amyloid-beta peptide aggregation, besides providing metal (Fe, Cu) chelating ability and concomitant extra anti-oxidant activity, for the hybrids with hydroxyl substitution. The new TAC-BF conjugates showed very good activity for AChE inhibition (sub-micromolar range) and good capacity for the inhibition of self- and Cu-mediated Aβ aggregation, with dependence on the linker size and substituent groups of each main moiety. Neuroprotective effects were also found for the compounds through viability assays of neuroblastoma cells, after Aβ
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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.