1.
Bioorg Med Chem Lett
; 12(7): 1099-102, 2002 Apr 08.
Artículo
en Inglés
| MEDLINE
| ID: mdl-11909726
RESUMEN
NMDA antagonists derived from 5-phosphonomethyl-1,4-dihydroquinoxaline-2,3-dione (3a) are potent anticonvulsant agents, and display strong protective effects in the electroshock-induced convulsion assay in mice. Their preference for the human NMDAR 1A/2A over 1A/2B subunit composition was optimized, leading to (1RS,1'S)-PEAQX (9r), which shows a >100-fold selectivity.