Kynurenic acid amides as novel NR2B selective NMDA receptor antagonists.
A novel series of kynurenic acid amides, ring-enlarged derivatives of indole-2-carboxamides, was prepared and identified as in vivo active NR2B subtype selective NMDA receptor antagonists. The synthesis and SAR studies are discussed.
Borza
István
I
Gedeon Richter Ltd, Budapest 10, PO Box 27, H-1475, Hungary. i.borza@richter.hu
Kolok
Sándor
S
Galgóczy
Kornél
K
Gere
Anikó
A
Horváth
Csilla
C
Farkas
Sándor
S
Greiner
István
I
Domány
György
G
D000577:Amides / Q000138:chemical synthesis / Q000494:pharmacology; D000700:Analgesics / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D001665:Binding Sites; D002851:Chromatography, High Pressure Liquid; D005557:Formaldehyde; D007202:Indicators and Reagents; D007736:Kynurenic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D010147:Pain Measurement / Q000187:drug effects; D010880:Piperidines / Q000378:metabolism; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
D000577:Amides; D000700:Analgesics; D007202:Indicators and Reagents; C121001:NR2B NMDA receptor; D010880:Piperidines; D016194:Receptors, N-Methyl-D-Aspartate; D005557:Formaldehyde; D007736:Kynurenic Acid; C010739:ifenprodil