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.
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
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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 |
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