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

A novel series of indole-2-carboxamide derivatives was prepared and identified as NR2B selective NMDA receptor antagonists. The influence of the number and position of OH groups on the indole skeleton as well as the substitution of the piperidine ring on the biological activity of the compounds was...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-11, Vol.13 (21), p.3859-3861
Hauptverfasser:	BORZA, Istvan, KOLOK, Sandor, BIELIK, Attila, NAGY, Jozsef, FARKAS, Sandor, DOMANY, György, GERE, Aniko, AGAI-CSONGOR, Eva, AGAI, Béla, TARKANYI, Gabor, HORVATH, Csilla, BARTA-SZALAI, Gizella, BOZO, Eva, KISS, Csilla
Format:	Artikel
Sprache:	eng
Schlagworte:	Binding, Competitive - drug effects Biological and medical sciences Excitatory Amino Acid Antagonists - pharmacology Glutamatergic system (aspartate and other excitatory aminoacids) Indoles - chemical synthesis Indoles - chemistry Indoles - pharmacology Magnetic Resonance Spectroscopy Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Phenols - pharmacology Piperidines - pharmacology Radioligand Assay Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors Spectrophotometry, Infrared Structure-Activity Relationship
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Zusammenfassung:	A novel series of indole-2-carboxamide derivatives was prepared and identified as NR2B selective NMDA receptor antagonists. The influence of the number and position of OH groups on the indole skeleton as well as the substitution of the piperidine ring on the biological activity of the compounds was studied.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(03)00708-X