Abstract
Background: Medicinal chemistry methodologies are presently used to develop multifunctional molecules which simultaneously reduce oxidative stress, excitotoxicity, metal dyshomeostasis, and neuroinflammation that characterize neuropathological conditions, such as Alzheimer’s Disease.
Results: Memantine (MEM) derivatives 1-6 were designed and synthesized as novel multifunctional entities with antioxidant and neuroprotective capabilities to manage neurodegenerative diseases, such as Alzheimer’s Disease. In vitro neuroprotective studies were performed by using astroglial GL15 cell line to assess antioxidant capability of MEM derivatives 1-6. Conclusion: Our outcomes showed that compounds 1 and 5 (at the concentration of 10 μM), containing as antioxidant portion residues of N-acetyl-Cys-OH and N-acetyl-Cys(Allyl)-OH, respectively, revealed a significant neuroprotective activity against oxidative stress, as assessed by NBT assays.Keywords: Alzheimer's disease, cysteine derivatives, MEM, neuroprotective, NMDA antagonist, S-Allylcysteine.
Graphical Abstract
Central Nervous System Agents in Medicinal Chemistry
Title:Synthesis and Antioxidant Properties of Novel Memantine Derivatives
Volume: 17 Issue: 2
Author(s): Erika Fornasari, Lisa Marinelli, Antonio Di Stefano, Piera Eusepi, Hasan Turkez, Stefania Fulle, Ester S. Di Filippo, Andrea Scarabeo, Silvia Di Nicola and Ivana Cacciatore*
Affiliation:
- Department of Pharmacy, University ,Italy
Keywords: Alzheimer's disease, cysteine derivatives, MEM, neuroprotective, NMDA antagonist, S-Allylcysteine.
Abstract: Background: Medicinal chemistry methodologies are presently used to develop multifunctional molecules which simultaneously reduce oxidative stress, excitotoxicity, metal dyshomeostasis, and neuroinflammation that characterize neuropathological conditions, such as Alzheimer’s Disease.
Results: Memantine (MEM) derivatives 1-6 were designed and synthesized as novel multifunctional entities with antioxidant and neuroprotective capabilities to manage neurodegenerative diseases, such as Alzheimer’s Disease. In vitro neuroprotective studies were performed by using astroglial GL15 cell line to assess antioxidant capability of MEM derivatives 1-6. Conclusion: Our outcomes showed that compounds 1 and 5 (at the concentration of 10 μM), containing as antioxidant portion residues of N-acetyl-Cys-OH and N-acetyl-Cys(Allyl)-OH, respectively, revealed a significant neuroprotective activity against oxidative stress, as assessed by NBT assays.Export Options
About this article
Cite this article as:
Fornasari Erika, Marinelli Lisa, Di Stefano Antonio, Eusepi Piera, Turkez Hasan, Fulle Stefania, Di Filippo S. Ester, Scarabeo Andrea, Di Nicola Silvia and Cacciatore Ivana*, Synthesis and Antioxidant Properties of Novel Memantine Derivatives, Central Nervous System Agents in Medicinal Chemistry 2017; 17 (2) . https://dx.doi.org/10.2174/1871524916666160625123621
DOI https://dx.doi.org/10.2174/1871524916666160625123621 |
Print ISSN 1871-5249 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6166 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Retinal Nerve Fiber Layer Thickness is Associated with Episodic Memory Deficit in Mild Cognitive Impairment Patients
Current Alzheimer Research A Review of Lysergic Acid Diethylamide (LSD) in the Treatment of Addictions: Historical Perspectives and Future Prospects
Current Drug Abuse Reviews The Expression of Relaxin-3 in Adipose Tissue and its Effects on Adipogenesis
Protein & Peptide Letters Restoring Sexual Desire After Surgical Menopause: Update on Assessment and Management
Current Women`s Health Reviews Acetylcholinesterase-Amyloid-β-peptide Interaction: Effect of Congo Red and the Role of the Wnt Pathway
Current Alzheimer Research Targeting the Bombesin/Gastrin-Releasing Peptide Receptor to Treat Sepsis
Recent Patents on Anti-Infective Drug Discovery Management of Early Stage Chronic Myeloid Leukemia: State-of-the-art Approach and Future Perspectives
Current Cancer Drug Targets Persistent Current Blockers of Voltage-Gated Sodium Channels: A Clinical Opportunity for Controlling Metastatic Disease
Recent Patents on Anti-Cancer Drug Discovery Remodeling Chromatin and Stress Resistance in the Central Nervous System: Histone Deacetylase Inhibitors as Novel and Broadly Effective Neuroprotective Agents
Current Drug Targets - CNS & Neurological Disorders Neuro-Inflammatory Mechanisms in Developmental Disorders Associated with Intellectual Disability and Autism Spectrum Disorder: A Neuro- Immune Perspective
CNS & Neurological Disorders - Drug Targets Neurotrophic Actions of Mood-Stabilizers: A Recent Research Discovery and its Potential Clinical Applications
Current Psychiatry Reviews Multifunctional Proteins in Tumorigenesis: Aminoacyl-tRNA Synthetases and Translational Components
Current Proteomics Synthesis and Biological Evaluation of 2´-Hydroxy-4´,6´-Diprenyloxychal-Cone Derivatives as Potent CDC25B and PTP1B Inhibitors
Letters in Drug Design & Discovery Editorial [PET and SPECT in Drug Evaluation and Drug Design: Novel Techniques]
Current Pharmaceutical Design New Approaches in the Treatment of Overactive Bladder: Targeting Adrenergic Receptors and Neurokinin Receptors
Current Medicinal Chemistry - Central Nervous System Agents Drug Metabolism in Chronic Renal Failure
Current Drug Metabolism Editorial from Guest Editor [Hot Topic:Animal Venoms: From Deadly Arsenals (Toxins) to Therapeutic Drug Candidates (Guest Editor: Jean-Marc Sabatier)]
Inflammation & Allergy - Drug Targets (Discontinued) Recent Development in Liquid Chromatography/Mass Spectrometry and Emerging Technologies for Metabolite Identification
Current Drug Metabolism The Start of a New Era for Stroke Treatment: Mechanical Thrombectomy Devices
Current Neurovascular Research Early Stage Identification of Alzheimer’s Disease Using a Two-stage Ensemble Classifier
Current Bioinformatics