N-phosphonoalkyl-5-aminomethylquinoxaline-2, 3-diones: in vivo active AMPA and NMDA (glycine) antagonists

YP Auberson, P Acklin, S Bischoff, R Moretti…

Index: Auberson, Yves P.; Acklin, Pierre; Bischoff, Serge; Moretti, Robert; Ofner, Silvio; Schmutz, Markus; Veenstra, Siem J. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 2 p. 249 - 254

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Citation Number: 45

Abstract

N-Substituted 5-aminomethylquinoxalinediones containing carboxy or phosphonic acids yield potent and selective AMPA and/or NMDA (glycine-binding site) antagonists. Phosphonic acid derivatives are particularly water-soluble and display potent anticonvulsant effects in the electroshock-induced convulsion assay in mice.