Synthesis and Antioxidant Properties of Novel Memantine Derivatives

Author(s): Erika Fornasari, Lisa Marinelli, Antonio Di Stefano, Piera Eusepi, Hasan Turkez, Stefania Fulle, Ester S. Di Filippo, Andrea Scarabeo, Silvia Di Nicola, Ivana Cacciatore*

Journal Name: Central Nervous System Agents in Medicinal Chemistry
Formerly Current Medicinal Chemistry - Central Nervous System Agents

Volume 17 , Issue 2 , 2017

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Graphical 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.

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Article Details

Year: 2017
Page: [123 - 128]
Pages: 6
DOI: 10.2174/1871524916666160625123621
Price: $65

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