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ID: ALA1130765

Journal: Bioorg Med Chem Lett

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

Authors: Acklin P, Allgeier H, Auberson YP, Bischoff S, Ofner S, Sauer D, Schmutz M.

Abstract: A series of quinoxaline-2,3-diones with very high affinity to the glycine site of the NMDA receptor has been discovered. In contrast to the 7-nitro derivatives, the most potent 7-bromo substituted compounds were highly selective for the glycine site. Although none of the described compounds were active in the electroshock model in mice, 1a displayed significant protection in the quinolinic acid-induced excitotoxicity model in vivo.

CiteXplore: 9871605

DOI: 10.1016/s0960-894x(98)00055-9