title: Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.
abstract: 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.
authors.affiliation: Gedeon Richter Ltd., Budapest, Hungary. i.borza@richter.hu
authors.forename: István
authors.initials: I
authors.lastname: Borza
authors.forename: Sándor
authors.initials: S
authors.lastname: Kolok
authors.forename: Anikó
authors.initials: A
authors.lastname: Gere
authors.forename: József
authors.initials: J
authors.lastname: Nagy
authors.forename: László
authors.initials: L
authors.lastname: Fodor
authors.forename: Kornél
authors.initials: K
authors.lastname: Galgóczy
authors.forename: József
authors.initials: J
authors.lastname: Fetter
authors.forename: Ferenc
authors.initials: F
authors.lastname: Bertha
authors.forename: Béla
authors.initials: B
authors.lastname: Agai
authors.forename: Csilla
authors.initials: C
authors.lastname: Horváth
authors.forename: Sándor
authors.initials: S
authors.lastname: Farkas
authors.forename: György
authors.initials: G
authors.lastname: Domány
mesh_terms: 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
chemical_list: D000577:Amides; D001562:Benzimidazoles; C121001:NR2B NMDA receptor; D016194:Receptors, N-Methyl-D-Aspartate; C031000:benzimidazole