Indole-2-carboxamidines as novel NR2B selective NMDA receptor antagonists

István Borza; Sándor Kolok; Györgyi Ignácz-Szendrei; István Greiner; Gábor Tárkányi; Kornél Galgóczy; Csilla Horváth; Sándor Farkas; György Domány

doi:10.1016/j.bmcl.2005.08.110

Indole-2-carboxamidines as novel NR2B selective NMDA receptor antagonists

Bioorg Med Chem Lett. 2005 Dec 15;15(24):5439-41. doi: 10.1016/j.bmcl.2005.08.110. Epub 2005 Oct 5.

Authors

István Borza¹, Sándor Kolok, Györgyi Ignácz-Szendrei, István Greiner, Gábor Tárkányi, Kornél Galgóczy, Csilla Horváth, Sándor Farkas, György Domány

Affiliation

¹ Gedeon Richter Ltd., Budapest, 10. PO Box 27, H-1475, Hungary. i.borza@richter.hu

PMID: 16213709
DOI: 10.1016/j.bmcl.2005.08.110

Abstract

A novel series of indole-2-carboxamidine derivatives was prepared and identified as NR2B selective NMDA receptor antagonists. The influence of the substituents on the indole skeleton as well as the substitution of the benzyl moiety on the biological activity of the compounds was studied. Compound 5a was po active in the formalin test in mouse.

MeSH terms

Aminoimidazole Carboxamide / chemical synthesis
Aminoimidazole Carboxamide / pharmacology*
Animals
Calcium / metabolism
Cell Culture Techniques
Cerebral Cortex / cytology
Cerebral Cortex / physiology
Imidazoles / chemical synthesis
Imidazoles / pharmacology*
Indoles / chemical synthesis
Indoles / pharmacology*
N-Methylaspartate / pharmacology*
Rats
Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*

Substances

Imidazoles
Indoles
NR2B NMDA receptor
Receptors, N-Methyl-D-Aspartate
Aminoimidazole Carboxamide
N-Methylaspartate
Calcium