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

Abstract
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 difference of activity observed in vitro, they shown similar neuroprotective profile in the MCAo model in rats.
AuthorsRomano Di Fabio, Elvira Tranquillini, Barbara Bertani, Giuseppe Alvaro, Fabrizio Micheli, Fabio Sabbatini, Maria Domenica Pizzi, Giorgio Pentassuglia, Alessandra Pasquarello, Tommaso Messeri, Daniele Donati, Emiliangelo Ratti, Roberto Arban, Giovanna Dal Forno, Angelo Reggiani, Robert J Barnaby
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 13 Issue 21 Pg. 3863-6 (Nov 03 2003) ISSN: 0960-894X [Print] England
PMID14552796 (Publication Type: Journal Article)
Chemical References
  • Neuroprotective Agents
  • Quinolines
  • Receptors, Glycine
  • Receptors, N-Methyl-D-Aspartate
Topics
  • Animals
  • Binding Sites
  • Brain Ischemia (drug therapy, pathology)
  • Dose-Response Relationship, Drug
  • Injections, Intravenous
  • Middle Cerebral Artery
  • Molecular Conformation
  • Neuroprotective Agents (chemical synthesis, pharmacology)
  • Quinolines (chemical synthesis, pharmacology)
  • Rats
  • Receptors, Glycine (antagonists & inhibitors)
  • Receptors, N-Methyl-D-Aspartate (antagonists & inhibitors)
  • Stereoisomerism

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