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http://hdl.handle.net/2445/179449
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DC Field | Value | Language |
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dc.contributor.author | Pereira, Nuno A. L. | - |
dc.contributor.author | Sureda, Francesc X. | - |
dc.contributor.author | Turch, Mireia | - |
dc.contributor.author | Amat Tusón, Mercedes | - |
dc.contributor.author | Bosch Cartes, Joan | - |
dc.contributor.author | Santos, Maria M. M. | - |
dc.date.accessioned | 2021-07-29T07:04:03Z | - |
dc.date.available | 2021-07-29T07:04:03Z | - |
dc.date.issued | 2013-01-09 | - |
dc.identifier.issn | 0026-9247 | - |
dc.identifier.uri | http://hdl.handle.net/2445/179449 | - |
dc.description.abstract | N-Methyl-D-aspartate (NMDA) receptor antagonists are known to rescue neuronal cell death caused by excessive activation of glutamate receptors. This phenomenon, known as excitotoxicity, is implicated in the pathogenesis of several neurodegenerative disorders including ischemia, Alzheimer's disease, Parkinson's disease, and Huntington's disease. Unfortunately, some NMDA receptor antagonists have shown discouraging results when tested in clinical trials. However, recent advances in the physiology and pharmacology of the NMDA receptor have kept interest alive in modulating NMDA receptors for therapeutic intervention. We present here the synthesis of a small library of phenylalaninol-derived oxazolopyrrolidone lactams and their evaluation as NMDA receptor antagonists. The compounds were easily synthesized in yields up to 92 %. In addition, one of the compounds has a 50 % inhibitory concentration (IC 50) of 62 μM and offers potential to develop more potent NMDA receptor antagonists. | - |
dc.format.extent | 5 p. | - |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | Springer Verlag | - |
dc.relation.isformatof | Versió postprint del document publicat a: https://doi.org/10.1007/s00706-012-0880-8 | - |
dc.relation.ispartof | Monatshefte für Chemie, 2013, vol. 144, num. 4, p. 473-477 | - |
dc.relation.uri | https://doi.org/10.1007/s00706-012-0880-8 | - |
dc.rights | (c) Springer Verlag, 2013 | - |
dc.source | Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) | - |
dc.subject.classification | Lactames | - |
dc.subject.classification | Receptors cel·lulars | - |
dc.subject.classification | Malalties neurodegeneratives | - |
dc.subject.other | Lactams | - |
dc.subject.other | Cell receptors | - |
dc.subject.other | Neurodegenerative Diseases | - |
dc.title | Synthesis of phenylalaninol-derived oxazolopyrrolidone lactams and evaluation as NMDA receptor antagonists | - |
dc.type | info:eu-repo/semantics/article | - |
dc.type | info:eu-repo/semantics/acceptedVersion | - |
dc.identifier.idgrec | 622326 | - |
dc.date.updated | 2021-07-29T07:04:03Z | - |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | - |
Appears in Collections: | Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) |
Files in This Item:
File | Description | Size | Format | |
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622326.pdf | 498.49 kB | Adobe PDF | View/Open |
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