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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 biol...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006-09, Vol.16 (17), p.4638-4640
Main Authors: Borza, István, Kolok, Sándor, Gere, Anikó, Nagy, József, Fodor, László, Galgóczy, Kornél, Fetter, József, Bertha, Ferenc, Ágai, Béla, Horváth, Csilla, Farkas, Sándor, Domány, György
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Language:English
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Summary: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. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.06.002