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

• Published in: Bioorganic & medicinal chemistry letters Vol. 13; no. 21; pp. 3859 - 3861
• Main Authors: 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: Journal Article
• Language: English
• Published: Oxford Elsevier 03.11.2003
• Subjects: 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; Nitrogen heterocycle; Glutamate receptor; Selectivity; In vitro; Structure activity relation; Piperidine derivatives; Bicyclic compound; Phenols; Carboxamide; Aromatic compound; Antagonist; Indole derivatives; NMDA receptor; Chemical synthesis
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/S0960-894X(03)00708-X

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.