3'-(Arylmethyl)- and 3'-(Aryloxy)-3-phenyl-4-hydroxyquinolin- 2(1H)-ones: Orally Active Antagonists of the Glycine Site on the NMDA Receptor
β Scribed by Kulagowski, Janusz J.; Baker, Raymond; Curtis, Neil R.; Mawer, Ian M.; Moseley, Angela M.; Ridgill, Mark P.; Rowley, Michael; Stansfield, Ian; Leeson, Paul D.
- Book ID
- 118270950
- Publisher
- American Chemical Society
- Year
- 1994
- Tongue
- English
- Weight
- 479 KB
- Volume
- 37
- Category
- Article
- ISSN
- 0022-2623
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A series of substituted 3-hydroxy-quinolin-2-one derivatives 6 was synthesized and evaluated as inhibitors of [3H]-glycine and [3H]-AMPA binding to rat cortical membranes. These compounds were generally found to be more potent ligands for the NMDA-associated glycine binding site than the AMPA recept
A short and efficient synthesis of the NMDA glycine site antagonist: (3R,4R)-3-amino-1-hydroxy-4methyl pyrrolidin-2-one (L-687,414) is described.