Author, as appears in the article.: Pereira, N.A.L. Sureda, F.X. Esplugas, R. Pérez, M. Amat, M. Santos, M.M.M.
Department: Ciències Mèdiques Bàsiques
e-ISSN: 1464-3405
URV's Author/s: Nuno A. L. Pereira, Francesc X. Sureda, Roser Esplugas, Maria Pérez, Mercedes Amat and Maria M. M. Santos
Abstract: N-Methyl-d-aspartate receptors (NMDAR) exacerbated activation leads to neuron death through a phenomenon called excitotoxicity. These receptors are implicated in several neurological diseases (e.g., Alzheimer and Parkinson) and thus represent an important therapeutic target. We herein describe the study of enantiopure tryptophanol-derived oxazolopiperidone lactams as NMDA receptor antagonists. The most active hit exhibited an IC50 of 63.4 µM in cultured rat cerebellar granule neurons thus being 1.5 fold more active than clinically approved NMDA antagonist amantadine (IC50 = 92 µM)
licence for use: https://creativecommons.org/licenses/by/3.0/es/
Keyword in other language: Amantadine lactam tryptophanol derived oxazolopiperidone lactam derivative unclassified drug degenerative disease
ISSN: 0960-894X
Last page: 3336
Journal volume: 24
Papper version: info:eu-repo/semantics/submittedVersion
Link to the original source: http://www.sciencedirect.com/science/article/pii/S0960894X14006349
Article's DOI: https://doi.org/10.1016/j.bmcl.2014.05.105
Entity: Universitat Rovira i Virgili.
Journal publication year: 2014
First page: 3333
Repositori URV