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Tricyclic quinoxalinediones, aza-kynurenic acids, and indole-2-carboxylic acids as in vivo active NMDA-glycine antagonists.

Abstract
This review article describes the development of in vivo active antagonists for the glycine binding site of the N-Methyl-D-Aspartate (NMDA) receptor. There were several difficulties in identifying a class of antagonists with in vivo efficacy and only a few compounds succeeded in emerging with activity in vivo. A series of tricyclic quinoxalinediones was highly potent glycine antagonists in vitro and the derivatives having a zwitterionic moiety including SM-18400 indeed showed in vivo activity. Similarly, tricyclic indole-2-carboxylic acids having a zwitterionic moiety such as SM-31900 were also active in vivo. In fact, SM-18400 and SM-31900 exhibited efficacy in several animal stroke models using intravenous infusion protocols. The practical syntheses of SM-18400 and SM-31900 as well as the novel synthesis of moderately active glycine antagonists, tricyclic azakynurenic acids, were also developed.
AuthorsRyu Nagata, Seiji Katayama, Ken-Ichi Ohtani, Hiroyasu Tanaka, Kozo Shimago
JournalCurrent topics in medicinal chemistry (Curr Top Med Chem) Vol. 6 Issue 7 Pg. 733-45 ( 2006) ISSN: 1568-0266 [Print] Netherlands
PMID16719813 (Publication Type: Journal Article, Review)
Chemical References
  • Indoles
  • Quinoxalines
  • Receptors, Glycine
  • indole-2-carboxylic acid
  • Kynurenic Acid
Topics
  • Indoles (chemical synthesis, chemistry, pharmacology)
  • Kynurenic Acid (chemical synthesis, chemistry, pharmacology)
  • Models, Molecular
  • Quinoxalines (chemical synthesis, chemistry, pharmacology)
  • Receptors, Glycine (antagonists & inhibitors)
  • Structure-Activity Relationship

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