5-Aminomethylquinoxaline-2,3-diones. Part II: N-aryl derivatives as novel NMDA/glycine and AMPA antagonists

Y P Auberson; P Acklin; H Allgeier; M Biollaz; S Bischoff; S Ofner; S J Veenstra

doi:10.1016/s0960-894x(97)10187-1

5-Aminomethylquinoxaline-2,3-diones. Part II: N-aryl derivatives as novel NMDA/glycine and AMPA antagonists

Bioorg Med Chem Lett. 1998 Jan 6;8(1):71-4. doi: 10.1016/s0960-894x(97)10187-1.

Authors

Y P Auberson¹, P Acklin, H Allgeier, M Biollaz, S Bischoff, S Ofner, S J Veenstra

Affiliation

¹ Novartis Pharma AG, Basel, Switzerland. [email protected]

PMID: 9871631
DOI: 10.1016/s0960-894x(97)10187-1

Abstract

Potent antagonists at the glycine-binding site of NMDA receptors, as well as dual antagonists acting also at AMPA receptors have been identified in a series of 5-arylaminomethylquinoxaline-2,3-diones. A study of the structure-activity relationship of these compounds is reported here.

MeSH terms

Excitatory Amino Acid Antagonists / chemistry
Excitatory Amino Acid Antagonists / metabolism
Excitatory Amino Acid Antagonists / pharmacology*
Glycine / metabolism*
Quinoxalines / chemistry
Quinoxalines / metabolism
Quinoxalines / pharmacology*
Receptors, AMPA / antagonists & inhibitors*
Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*
Receptors, N-Methyl-D-Aspartate / chemistry
Structure-Activity Relationship

Substances

Excitatory Amino Acid Antagonists
Quinoxalines
Receptors, AMPA
Receptors, N-Methyl-D-Aspartate
Glycine