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BIBTEX RIS

Stereoselective synthesis and preliminary evaluation of new d-3-heteroarylcarbonylalanines as ligands of the NMDA receptor

2004; Elsevier BV; Volume: 14; Issue: 17 Linguagem: Inglês

10.1016/j.bmcl.2004.06.062

1464-3405

Paulo G. de Lima, Rodrigo Rêgo Barros Caruso, Simone O. Alves, Renata Fittipaldi Pessôa, Dayde Lane Mendonça da Silva, Ricardo José Nunes, François Noël, Newton G. Castro, Paulo R. R. Costa,

Molecular Sensors and Ion Detection

New N-heteroarylcarbonylalanines of the d-series were stereoselectively prepared from enoates derived from d-mannitol. These compounds were active in binding and functional assays of the NMDA sub-type of glutamate receptors. A pyridine derivative inhibited MK801 binding, protected neurons from excitotoxic damage and blocked NMDA-induced currents in neurons. A thiophene derivative positively modulated the NMDA receptor, possibly through the allosteric glycine site.