PMID

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Article Title

Organization

Unusual synthesis of new glycine antagonists via sequential aldol condensation-lactonization-elimination reaction.

Glaxowellcome

The glutamate receptor GluR5 agonist (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid and the 8-methyl analogue: synthesis, molecular pharmacology, and biostructural characterization.

University of Copenhagen

Enantiomeric propanolamines as selective N-methyl-D-aspartate 2B receptor antagonists.

Emory University

N-Hydroxypyrazolyl glycine derivatives as selective N-methyl-D-aspartic acid receptor ligands.

University of Copenhagen

2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.

Universit£

Design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine sigma ligands as potential antipsychotic drugs.

Taisho Pharmaceutical

Synthesis of 1,4,7,8,9,10-hexahydro-9-methyl-6-nitropyrido[3,4-f]- quinoxaline-2,3-dione and related quinoxalinediones: characterization of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (and N-methyl-D-aspartate) receptor and anticonvulsant activity.

Warner-Lambert

Synthesis and excitatory amino acid pharmacology of a series of heterocyclic-fused quinoxalinones and quinazolinones.

Eli Lilly

Synthesis and structure-activity relationship of C5-substituted analogues of (+-)-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine [(+-)-desmethyl-MK801]: ligands for the NMDA receptor-coupled phencyclidine binding site.

National Institute of Diabetes and Digestive and Kidney Diseases

5-Aminomethylquinoxaline-2,3-diones, Part III: Arylamide derivatives as highly potent and selective glycine-site NMDA receptor antagonists.

Novartis Pharma

5-Aminomethylquinoxaline-2,3-diones. Part I: A novel class of AMPA receptor antagonists.

Novartis Pharma

 

Synthesis and glutamate antagonist activity of 4-phosphonoalkylquinoline derivatives: A novel class of non-NMDA antagonist

TBA

 

Synthesis and excitatory amino acid pharmacology of some novel quinoxalinediones

TBA

3-(aminomethyl)piperazine-2,5-dione as a novel NMDA glycine site inhibitor from the chemical universe database GDB.

University of Berne

 

6,7,8,9-tetrahydro-3-hydroxy-1H-1-benzazepine-2,5-diones via a diels-alder reaction:antagonists with a non-planar hydrophobic region for NMDA receptor glycine sites

TBA

 

Tetramic acids as novel glycine site antagonists

TBA

 

5,6,7,8-Tetrahydroquinolones as antagonists at the glycine site of the NMDA receptor

TBA

 

Structure-activity relationships of tricyclic quinoxalinediones as potent antagonists for the glycine binding site of the NMDA receptor 2

TBA

 

Structure-activity relationships of tricyclic quinoxalinediones as potent antagonists for the glycine binding site of the NMDA receptor 1

TBA

 

NS 257 (1,2,3,6,7,8-hexahydro-3(hydroxyimino)-N,N,7-trimethyl-2-oxobenzo[2,1-b:3,4-c']dipyrrole-5-sulfonamide) is a potent, systemically active ampa receptor antagonist

TBA

 

Structure-activity relationships of a series of glycine antagonists related to 5,7-dichlorokynurenic acid and 3-(2-carboxy-6-chloroindol-3-yl)acetic acid

TBA

 

Derivatives of 1-hydroxy-3-aminopyrrolidin-2-one (HA-966). Partial agonists at the glycine site of the NMDA receptor

TBA

 

2-carboxy indolines and indoles as potential glycine/NMDA antagonists: effect of five-membered ring conformation on affinity.

TBA

 

Design, synthesis and molecular modeling of 3-acylamino-2- Carboxyindole NMDA receptor glycine-site antagonists

TBA

 

Tricyclic quinoxalines as ligands for the strychnine-insensitive glycine site

TBA

Synthesis and biological evaluation of 1-amino-2-phosphonomethylcyclopropanecarboxylic acids, new group III metabotropic glutamate receptor agonists.

University Paris Descartes

3-hydroxy-quinazoline-2,4-dione as a useful scaffold to obtain selective Gly/NMDA and AMPA receptor antagonists.

Universita Degli Studi Di Firenze

Synthesis and biological evaluation of analogues of 7-chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid (TQX-173) as novel selective AMPA receptor antagonists.

Universita Degli Studi Di Firenze

Selectivity fields: comparative molecular field analysis (CoMFA) of the glycine/NMDA and AMPA receptors.

Moscow State University

Tricyclic indole-2-carboxylic acids: highly in vivo active and selective antagonists for the glycine binding site of the NMDA receptor.

Sumitomo Pharmaceuticals

Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists.

Università

Synthesis and biological evaluation of a new set of pyrazolo[1,5-c]quinazoline-2-carboxylates as novel excitatory amino acid antagonists.

Universita' Di Firenze

Evaluation and biological properties of reactive ligands for the mapping of the glycine site on the N-methyl-D-aspartate (NMDA) receptor.

Université

4,5-Dihydro-1,2,4-triazolo[1,5-a]quinoxalin-4-ones: excitatory amino acid antagonists with combined glycine/NMDA and AMPA receptor affinity.

Universita' Di Firenze

Design, synthesis and structure-activity relationships of novel strychnine-insensitive glycine receptor ligands.

Institut De Recherches Servier

(E)-3-(2-(N-phenylcarbamoyl)vinyl)pyrrole-2-carboxylic acid derivatives. A novel class of glycine site antagonists.

Università

5-(N-oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: novel, systemically active and broad spectrum antagonists for NMDA/glycine, AMPA, and kainate receptors.

Cocensys

Synthesis of racemic 6,7,8,9-tetrahydro-3-hydroxy-1H-1-benzazepine-2,5-diones as antagonists of N-methyl-d-aspartate (NMDA) and alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptors.

Cocensys

4-substituted-3-phenylquinolin-2(1H)-ones: acidic and nonacidic glycine site N-methyl-D-aspartate antagonists with in vivo activity.

Merck Sharp and Dohme Research Laboratories

Structure-activity relationships of alkyl- and alkoxy-substituted 1,4-dihydroquinoxaline-2,3-diones: potent and systemically active antagonists for the glycine site of the NMDA receptor.

Cocensys

Novel AMPA receptor antagonists: synthesis and structure-activity relationships of 1-hydroxy-7-(1H-imidazol-1-yl)-6-nitro-2,3(1H,4H)- quinoxalinedione and related compounds.

Yamanouchi Pharmaceutical

Synthesis and structure-activity relationships of 1,2,3,4-tetrahydroquinoline-2,3,4-trione 3-oximes: novel and highly potent antagonists for NMDA receptor glycine site.

Cocensys

Novel alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate receptor antagonists: synthesis and structure-activity relationships of 6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-pyrido[2,3-b]pyrazinedione and related compounds.

Yamanouchi Pharmaceutical

3-Nitro-3,4-dihydro-2(1H)-quinolones. Excitatory amino acid antagonists acting at glycine-site NMDA and (RS)-alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors.

Merck Sharp and Dohme Research Laboratories

3'-(Arylmethyl)- and 3'-(aryloxy)-3-phenyl-4-hydroxyquinolin-2(1H)-ones: orally active antagonists of the glycine site on the NMDA receptor.

Merck Sharp and Dohme Research Laboratories

Identification of 3,5-dihydro-2-aryl-1H-pyrazolo[3,4-c]quinoline-1,4(2H)-diones as novel high-affinity glycine site N-methyl-D-aspartate antagonists.

Merck Sharp and Dohme Research Laboratories

Resolution, absolute stereochemistry, and pharmacology of the S-(+)- and R-(-)-isomers of the apparent partial AMPA receptor agonist (R,S)-2-amino-3-(3-hydroxy-5-phenylisoxazol-4-yl)propionic acid [(R,S)-APPA].

Royal Danish School of Pharmacy

Substituted indole-2-carboxylates as in vivo potent antagonists acting as the strychnine-insensitive glycine binding site.

Glaxo Wellcome

Evaluation and synthesis of aminohydroxyisoxazoles and pyrazoles as potential glycine agonists.

Warner-Lambert

Synthesis, stereochemistry, and biological activity of the 1-(1-phenyl-2-methylcyclohexyl)piperidines and the 1-(1-phenyl-4-methylcyclohexyl)piperidines. Absolute configuration of the potent trans-(-)-1-(1-phenyl-2-methylcyclohexyl)piperidine.

Istituto Superiore Di Sanità

4-Amido-2-carboxytetrahydroquinolines. Structure-activity relationships for antagonism at the glycine site of the NMDA receptor.

Merck Sharp and Dohme Research Laboratories

3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site.

Marion Merrell Dow Research Institute

Synthesis, configuration, and activity of isomeric 2-phenyl-2-(N-piperidinyl)bicyclo[3.1.0]hexanes at phencyclidine and sigma binding sites.

National Institute of Diabetes and Digestive and Kidney Diseases

3-Phenyl-4-hydroxyquinolin-2(1H)-ones: potent and selective antagonists at the strychnine-insensitive glycine site on the N-methyl-D-aspartate receptor complex.

Eli Lilly

Beta-proline analogues as agonists at the strychnine-sensitive glycine receptor.

Warner-Lambert

Inhibition of HIV-1 Reverse Transcriptase Dimerization by Small Molecules.

University of Siena

Identifying New Drug Targets for Potent Phospholipase D Inhibitors: Combining Sequence Alignment, Molecular Docking, and Enzyme Activity/Binding Assays.

Roxbury Community College

Inhibition of the enzymatic activity of heme oxygenases by azole-based antifungal drugs.

Queen'S University