Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists

István Borza, Sándor Kolok, Anikó Gere, József Nagy, László Fodor, Kornél Galgóczy, J. Fetter, Ferenc Bertha, B. Ágai, Csilla Horváth, Sándor Farkas, György Domány

Research output: Contribution to journalArticle

17 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)4638-4640
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number17
DOIs
Publication statusPublished - Sep 1 2006

Fingerprint

N-Methyl-D-Aspartate Receptors
Pain Measurement
Bioactivity
Skeleton
Formaldehyde
Substitution reactions
Derivatives
benzimidazole
NR2B NMDA receptor
piperidine

Keywords

  • Benzimidazole
  • NMDA
  • NR2B

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Borza, I., Kolok, S., Gere, A., Nagy, J., Fodor, L., Galgóczy, K., ... Domány, G. (2006). Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists. Bioorganic and Medicinal Chemistry Letters, 16(17), 4638-4640. https://doi.org/10.1016/j.bmcl.2006.06.002

Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists. / Borza, István; Kolok, Sándor; Gere, Anikó; Nagy, József; Fodor, László; Galgóczy, Kornél; Fetter, J.; Bertha, Ferenc; Ágai, B.; Horváth, Csilla; Farkas, Sándor; Domány, György.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 16, No. 17, 01.09.2006, p. 4638-4640.

Research output: Contribution to journalArticle

Borza, I, Kolok, S, Gere, A, Nagy, J, Fodor, L, Galgóczy, K, Fetter, J, Bertha, F, Ágai, B, Horváth, C, Farkas, S & Domány, G 2006, 'Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists', Bioorganic and Medicinal Chemistry Letters, vol. 16, no. 17, pp. 4638-4640. https://doi.org/10.1016/j.bmcl.2006.06.002
Borza, István ; Kolok, Sándor ; Gere, Anikó ; Nagy, József ; Fodor, László ; Galgóczy, Kornél ; Fetter, J. ; Bertha, Ferenc ; Ágai, B. ; Horváth, Csilla ; Farkas, Sándor ; Domány, György. / Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists. In: Bioorganic and Medicinal Chemistry Letters. 2006 ; Vol. 16, No. 17. pp. 4638-4640.
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