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Cent Nerv Syst Agents Med Chem ; 17(2): 123-128, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-27356627

RESUMO

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.


Assuntos
Antioxidantes/síntese química , Antioxidantes/farmacologia , Astrócitos/efeitos dos fármacos , Memantina/síntese química , Memantina/farmacologia , Astrócitos/metabolismo , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/fisiologia , Antagonistas de Aminoácidos Excitatórios/síntese química , Antagonistas de Aminoácidos Excitatórios/farmacologia , Humanos
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