Utilize este identificador para referenciar este registo: http://hdl.handle.net/10451/17882
Título: Synthesis of phenylalaninol-derived oxazolopyrrolidone lactams and evaluation as NMDA receptor antagonists
Autor: Pereira, Nuno A. L.
Sureda, Francesc X.
Turch, M.
Amat, Mercedes
Bosch, Joan
Santos, Maria M. M.
Palavras-chave: Amino alcohols
Chiral auxiliaries
NMDA receptor antagonists
Pyrrolidones
Lactams
Data: 2013
Citação: Monatsh Chem (2013) 144:473–477
Resumo: 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 mu M and offers potential to develop more potent NMDA receptor antagonists.
Peer review: yes
URI: http://hdl.handle.net/10451/17882
DOI: http://dx.doi.org/10.1007/s00706-012-0880-8
Versão do Editor: The final publication is available at Springer via http://dx.doi.org/10.1007/s00706-012-0880-8
Aparece nas colecções:FF - Artigos em Revistas Internacionais

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