Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.
A novel series of benzimidazole-2-carboxamide derivatives was prepared and identified as NR2B selective NMDA receptor antagonists. The influence of some structural elements, like H-bond donor groups placed on the benzimidazole skeleton and the substitution pattern of the piperidine ring, on the biological activity was studied. Compound 6a showed excellent analgetic activity in the mouse formalin test following po administration.
Borza
István
I
Gedeon Richter Ltd., Budapest, Hungary. i.borza@richter.hu
Kolok
Sándor
S
Gere
Anikó
A
Nagy
József
J
Fodor
László
L
Galgóczy
Kornél
K
Fetter
József
J
Bertha
Ferenc
F
Agai
Béla
B
Horváth
Csilla
C
Farkas
Sándor
S
Domány
György
G
D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001562:Benzimidazoles / Q000737:chemistry*; D015394:Molecular Structure; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D013329:Structure-Activity Relationship
D000577:Amides; D001562:Benzimidazoles; C121001:NR2B NMDA receptor; D016194:Receptors, N-Methyl-D-Aspartate; C031000:benzimidazole