Repositori institucional URV
| URV's Author/s: | Nuno A. L. Pereira, Francesc X. Sureda, Roser Esplugas, Maria Pérez, Mercedes Amat and Maria M. M. Santos |
| Author, as appears in the article.: | Pereira, N.A.L. Sureda, F.X. Esplugas, R. Pérez, M. Amat, M. Santos, M.M.M. |
| Journal publication year: | 2014 |
| ISSN: | 0960-894X |
| e-ISSN: | 1464-3405 |
| 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) |
| Article's DOI: | https://doi.org/10.1016/j.bmcl.2014.05.105 |
| Link to the original source: | http://www.sciencedirect.com/science/article/pii/S0960894X14006349 |
| Papper version: | info:eu-repo/semantics/submittedVersion |
| licence for use: | https://creativecommons.org/licenses/by/3.0/es/ |
| Department: | Ciències Mèdiques Bàsiques |
| Licence document URL: | https://repositori.urv.cat/ca/proteccio-de-dades/ |
| Keyword in other language: | Amantadine lactam tryptophanol derived oxazolopiperidone lactam derivative unclassified drug degenerative disease |
| Entity: | Universitat Rovira i Virgili. |
| First page: | 3333 |
| Last page: | 3336 |
| Journal volume: | 24 |
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| DocumentPrincipal | DocumentPrincipal | application/pdf |
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