Stereoselective synthesis and preliminary evaluation of new D-3-heteroarylcarbonylalanines as ligands of the NMDA receptor |
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| Authors: | Lima Paulo G Caruso Rodrigo R B Alves Simone O Pessôa Renata F Mendonça-Silva Dayde L Nunes Ricardo J Noël François Castro Newton G Costa Paulo R R |
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| Institution: | Laboratório de Química Bioorganica, Núcleo de Pesquisas de Produtos Naturais, Centro de Ciências da Saúde, Bloco J, Universidade Federal do Rio de Janeiro, RJ 21941-590, Brazil. |
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| Abstract: | 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. |
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