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.
