ArticleMolecules (Basel, Switzerland)2020
Galantamine-Curcumin Hybrids as Dual-Site Binding Acetylcholinesterase Inhibitors.
Article in Molecules (Basel, Switzerland), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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The trial behind it
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Who cites it
23 citing papers in PubMed, 43 citations in OpenAlex.
- In Silico Isomerization Produces Apt Negative Data for VHTS Validation.Journal of chemical information and modeling · 2026Article
- Discovery ofRSC advances · 2026Article
- Boron Containing Curcumin-Like Compound as an Acetylcholinesterase Inhibitor and Anticancer Agent: Synthesis, Biological Evaluation, and Computational Insights.Cell biochemistry and biophysics · 2026Article
- Design and Physicochemical Characterization of Hybrid PLGA-Curcumin/Carbon Dot Nanoparticles for Sustained Galantamine Release: A Proof-of-Concept Study.Biomolecules · 2026Article
- An efficient computational chemistry approach to generating negative data for drug discovery pipeline validation.Frontiers in bioinformatics · 2026Article
- Acetylcholinesterase as a Multifunctional Target in Amyloid-Driven Neurodegeneration: From Dual-Site Inhibitors to Anti-Agregation Strategies.International journal of molecular sciences · 2025Review
- Esterified Indole-3-propionic Acid: A Novel Inhibitor against Cholinesterase Identified through Experimental and Computational Approaches.ACS omega · 2025Article
- Integrated Colorisensing Platform with Microneedles and Metal-Phenol Nanozymes for Point-of-Care Testings of Acetylcholinesterase Activity and Its Drug Inhibitor.International journal of nanomedicine · 2025Article
- Phytochemical and Cytotoxic Aspects of Amaryllidaceae Alkaloids inPlants (Basel, Switzerland) · 2024Review
- Review
- Molecular and Pharmacokinetic Aspects of the Acetylcholinesterase-Inhibitory Potential of the Oleanane-Type Triterpenes and Their Glycosides.Biomolecules · 2023Article
- Neuroprotective Properties of Oleanolic Acid-Computational-Driven Molecular Research Combined with In Vitro and In Vivo Experiments.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Unfolding the Antibacterial Activity and Acetylcholinesterase Inhibition Potential of Benzofuran-Triazole Hybrids: Synthesis, Antibacterial, Acetylcholinesterase Inhibition, and Molecular Docking Studies.Molecules (Basel, Switzerland) · 2023Article
- Photobiomodulation in Alzheimer's Disease-A Complementary Method to State-of-the-Art Pharmaceutical Formulations and Nanomedicine?Pharmaceutics · 2023Review
- Ex Vivo Antioxidant and Cholinesterase Inhibiting Effects of a Novel Galantamine-Curcumin Hybrid on Scopolamine-Induced Neurotoxicity in Mice.International journal of molecular sciences · 2022Article
- Virtual Screening and Hit Selection of Natural Compounds as Acetylcholinesterase Inhibitors.Molecules (Basel, Switzerland) · 2022Article
- Potential Therapeutic Applications of Plant-Derived Alkaloids against Inflammatory and Neurodegenerative Diseases.Evidence-based complementary and alternative medicine : eCAM · 2022Review
- The Potential Effect of Insulin on AChE and Its Interactions with Rivastigmine In Vitro.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Chronic Stress and Oxidative Stress as Common Factors of the Pathogenesis of Depression and Alzheimer's Disease: The Role of Antioxidants in Prevention and Treatment.Antioxidants (Basel, Switzerland) · 2021Review
- A Galantamine-Curcumin Hybrid Decreases the Cytotoxicity of Amyloid-Beta Peptide on SH-SY5Y Cells.International journal of molecular sciences · 2021Article
Corrections and comments
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Authors and funding
10 authors at 3 institutions in 2 countries.
Funding
Abstract
Galantamine (GAL) and curcumin (CU) are alkaloids used to improve symptomatically neurodegenerative conditions like Alzheimer's disease (AD). GAL acts mainly as an inhibitor of the enzyme acetylcholinesterase (AChE). CU binds to amyloid-beta (Aβ) oligomers and inhibits the formation of Aβ plaques. Here, we combine GAL core with CU fragments and design a combinatorial library of GAL-CU hybrids as dual-site binding AChE inhibitors. The designed hybrids are screened for optimal ADME properties and BBB permeability and docked on AChE. The 14 best performing compounds are synthesized and tested in vitro for neurotoxicity and anti-AChE activity. Five of them are less toxic than GAL and CU and show activities between 41 and 186 times higher than GAL.
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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.