Enantiomerically pure tetrahydroquinoline derivatives as in vivo potent antagonists of the glycine binding site associated to the NMDA receptor.

@article{Fabio2003EnantiomericallyPT,
  title={Enantiomerically pure tetrahydroquinoline derivatives as in vivo potent antagonists of the glycine binding site associated to the NMDA receptor.},
  author={Romano di Fabio and Elvira Tranquillini and Barbara Bertani and Giuseppe S Alvaro and Fabrizio Micheli and Fabio Maria Sabbatini and Maria Domenica Pizzi and Giorgio Pentassuglia and Alessandra Pasquarello and Tommaso Messeri and Daniele Donati and Emiliangelo A Ratti and Roberto Arban and Giovanna Dal Forno and Angelo Reggiani and Robert J Barnaby},
  journal={Bioorganic & medicinal chemistry letters},
  year={2003},
  volume={13 21},
  pages={3863-6}
}
To identify neuroprotective agents after stroke, new substituted tetrahydroquinoline derivatives were designed as antagonists of the glycine binding site associated to the NMDA receptor, satisfying the key pharmacophoric requirements. In particular, the racemate 3c exhibited outstanding in vivo activity in the MCAo model in rats, when given iv both pre- and post-ischemia. Pure enantiomers 3c-(+) and 3c-(-) have been prepared following an original synthetic route. Despite the significant… CONTINUE READING