Kynurenic acid amides as novel NR2B selective NMDA receptor antagonists

Starting from indole- and benzimidazole-2-carboxamides as lead compounds, a novel series of kynurenic acid amide derivatives was prepared and identified as NR2B selective NMDA receptor antagonists. The synthesis and SAR studies are discussed. A novel series of kynurenic acid amides, ring-enlarged de...

Full description

Saved in:

Bibliographic Details
Published in	Bioorganic & medicinal chemistry letters Vol. 17; no. 2; pp. 406 - 409
Main Authors	Borza, István, Kolok, Sándor, Galgóczy, Kornél, Gere, Anikó, Horváth, Csilla, Farkas, Sándor, Greiner, István, Domány, György
Format	Journal Article
Language	English
Published	Oxford Elsevier Ltd 15.01.2007 Elsevier
Subjects	Amides - chemical synthesis Amides - pharmacology Analgesics - chemical synthesis Analgesics - pharmacology Animals Binding Sites Biological and medical sciences Chromatography, High Pressure Liquid Formaldehyde Glutamatergic system (aspartate and other excitatory aminoacids) Indicators and Reagents Kynurenic Acid - analogs & derivatives Kynurenic Acid - chemical synthesis Kynurenic Acid - pharmacology Kynurenic acid amide Magnetic Resonance Spectroscopy Medical sciences Mice Neuropharmacology Neurotransmitters. Neurotransmission. Receptors NR2B antagonist Pain Measurement - drug effects Pharmacology. Drug treatments Piperidines - metabolism Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors Spectrophotometry, Infrared Structure-Activity Relationship NR2B antagonist Kynurenic acid amide Rodentia Oral administration Glutamate receptor Selectivity In vivo Vertebrata Ifenprodil Mammalia Structure activity relation Mouse Animal Organic fluorine compounds Piperidine derivatives Phenols Carboxamide Antagonist Indole derivatives NMDA receptor Chemical synthesis
Online Access	Get full text

Cover

Loading…

More Information
Summary:	Starting from indole- and benzimidazole-2-carboxamides as lead compounds, a novel series of kynurenic acid amide derivatives was prepared and identified as NR2B selective NMDA receptor antagonists. The synthesis and SAR studies are discussed. A novel series of kynurenic acid amides, ring-enlarged derivatives of indole-2-carboxamides, was prepared and identified as in vivo active NR2B subtype selective NMDA receptor antagonists. The synthesis and SAR studies are discussed.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.10.033