CoMFA, Synthesis, and Pharmacological Evaluation of (E)-3-(2-Carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic Acids: 3-[2-(3-Aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic Acid, a Potent Selective Glycine-Site NMDA Receptor Antagonist

(E)-3-(2-Carboxy-2-phenylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acid, 1, is a potent and selective antagonist of the glycine site of the N-methyl-d-aspartate (NMDA) receptor. Using 3D comparative molecular field analysis (CoMFA) to guide the synthetic effort, a series of aryl diacid analogues of...

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Veröffentlicht in:	Journal of medicinal chemistry 2005-02, Vol.48 (4), p.995-1018
Hauptverfasser:	Baron, Bruce M, Cregge, Robert J, Farr, Robert A, Friedrich, Dirk, Gross, Raymond S, Harrison, Boyd L, Janowick, David A, Matthews, Donald, McCloskey, Timothy C, Meikrantz, Scott, Nyce, Philip L, Vaz, Roy, Metz, William A
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anticonvulsants - chemical synthesis Anticonvulsants - chemistry Anticonvulsants - pharmacology Binding Sites Carboxylic Acids - chemical synthesis Carboxylic Acids - chemistry Carboxylic Acids - pharmacology Cyclic GMP - biosynthesis Glycine - metabolism In Vitro Techniques Indoles - chemical synthesis Indoles - chemistry Indoles - pharmacology Male Mice Mice, Inbred DBA Models, Molecular Neuroprotective Agents - chemical synthesis Neuroprotective Agents - chemistry Neuroprotective Agents - pharmacology Phenylacetates - chemical synthesis Phenylacetates - chemistry Phenylacetates - pharmacology Quantitative Structure-Activity Relationship Radioligand Assay Rats Rats, Sprague-Dawley Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors Receptors, N-Methyl-D-Aspartate - chemistry Seizures - etiology Seizures - prevention & control Stereoisomerism Stroke - drug therapy Stroke - pathology
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