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Title: Synthesis of phenylalaninol-derived oxazolopyrrolidone lactams and evaluation as NMDA receptor antagonists
Author: Pereira, Nuno A. L.
Sureda, Francesc X.
Turch, Mireia
Amat Tusón, Mercedes
Bosch Cartes, Joan
Santos, Maria M. M.
Keywords: Lactames
Receptors cel·lulars
Malalties neurodegeneratives
Cell receptors
Neurodegenerative Diseases
Issue Date: 9-Jan-2013
Publisher: Springer Verlag
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.
Note: Versió postprint del document publicat a:
It is part of: Monatshefte für Chemie, 2013, vol. 144, num. 4, p. 473-477
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ISSN: 0026-9247
Appears in Collections:Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica)

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