5-Aminomethylquinoxaline-2,3-diones. Part II: N-aryl derivatives as novel NMDA/glycine and AMPA antagonists.
Potent antagonists at the glycine-binding site of NMDA receptors, as well as dual antagonists acting also at AMPA receptors have been identified in a series of 5-arylaminomethylquinoxaline-2,3-diones. A study of the structure-activity relationship of these compounds is reported here.
Auberson
Y P
YP
Novartis Pharma AG, Basel, Switzerland. yves.auberson@pharma.novartis.com
Acklin
P
P
Allgeier
H
H
Biollaz
M
M
Bischoff
S
S
Ofner
S
S
Veenstra
S J
SJ
D018691:Excitatory Amino Acid Antagonists / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D005998:Glycine / Q000378:metabolism*; D011810:Quinoxalines / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors*; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013329:Structure-Activity Relationship
D018691:Excitatory Amino Acid Antagonists; D011810:Quinoxalines; D018091:Receptors, AMPA; D016194:Receptors, N-Methyl-D-Aspartate; D005998:Glycine