Indole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.
A novel series of indole-2-carboxamide derivatives was prepared and identified as NR2B selective NMDA receptor antagonists. The influence of the number and position of OH groups on the indole skeleton as well as the substitution of the piperidine ring on the biological activity of the compounds was studied.
Borza
István
I
Gedeon Richter Ltd., POB 27, H-1475 Budapest 10, Hungary. i.borza@richter.hu
Kolok
Sándor
S
Gere
Anikó
A
Agai-Csongor
Eva
E
Agai
Béla
B
Tárkányi
Gábor
G
Horváth
Csilla
C
Barta-Szalai
Gizella
G
Bozó
Eva
E
Kiss
Csilla
C
Bielik
Attila
A
Nagy
József
J
Farkas
Sándor
S
Domány
György
G
D001667:Binding, Competitive / Q000187:drug effects; D018691:Excitatory Amino Acid Antagonists / Q000494:pharmacology; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D010636:Phenols / Q000494:pharmacology; D010880:Piperidines / Q000494:pharmacology; D011869:Radioligand Assay; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
D018691:Excitatory Amino Acid Antagonists; D007211:Indoles; C121001:NR2B NMDA receptor; D010636:Phenols; D010880:Piperidines; D016194:Receptors, N-Methyl-D-Aspartate; C109643:Ro 25-6981