Design, synthesis and structure-activity relationships of novel strychnine-insensitive glycine receptor ligands.
The in vitro activities of 3-hydroxy-imidazolidin-4-one derivatives demonstrated very restricted structure-activity relationships at the strychnine-insensitive glycine site of the NMDA receptor. The most active compound (3a) was completely unsubstituted and exhibited affinity and efficacy similar to that of D-cycloserine, the prototypical partial agonist at this site.
Cordi
A
A
Institut de Recherches Servier, Suresnes, France. cordi@netgrs.com
Lacoste
J M
JM
Audinot
V
V
Millan
M
M
D015195:Drug Design; D005998:Glycine / Q000378:metabolism*; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008024:Ligands; D016194:Receptors, N-Methyl-D-Aspartate / Q000737:chemistry / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013331:Strychnine / Q000494:pharmacology*
C120091:3-hydroxyimidazolidin-4-one; D007093:Imidazoles; D008024:Ligands; D016194:Receptors, N-Methyl-D-Aspartate; D013331:Strychnine; D005998:Glycine