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Synthesis and Antioxidant Properties of Novel Memantine Derivatives

[ Vol. 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   Pages 123 - 128 ( 6 )

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.

Affiliation:

Department of Pharmacy, University , Department of Pharmacy, University , Department of Pharmacy, University , Department of Pharmacy, University , Department of Molecular Biology and Genetics, Faculty of Science, Erzurum Technical University, 25240, Erzurum, Department of Neuroscience and Imaging, University , Department of Neuroscience and Imaging, University , Dompé farmaceutici S.p.A., Via Campo di Pile, 67100 L'aquila (AQ), Dompé farmaceutici S.p.A., Via Campo di Pile, 67100 L'aquila (AQ), Department of Pharmacy, University

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