| abstract |
(57) [Summary] Formula (I) [Wherein, R is a group C = R 3, C (R 4) a R 5 or CH-R 6, R 1 and R 2 are hydrogen, halogen, alkyl, alkoxy, amino, acylamino, -NH-CO- NH-Ar, -N = CH- N (alk) alk ', nitro, cyano, phenyl, imidazolyl or SO 3 H, R 3 is oxygen, NOH, an NO-alk-COOX or CH-R 7, R 4 is alkyl, -alk-Het or -alk-Ar, R 5 is alkyl, or an -alk-Het or -alk-Ar, or C (R 4) R 5 is cycloalkyl, R 6 hydroxyalkyl, alkyl, -NR 8 R 9, -alk- OH, -alk-NR 8 R 9, a -alk-Ar or -alk-Het, R 7 is hydroxy, alkyl, phenyl, -alk-Ar a -alk-Het, NR 10 R 11 or a heterocyclic ring, R 8 and R 9 is alkyl , Or R 8 is and R 9 is hydrogen is hydrogen or alkyl, -COR 12, a -csr 30 or -SO 2 R 13, R 10 and R 11 is alkyl or cycloalkyl, R 12 is alkyl, cycloalkyl, phenyl, -COO-alk, -CH 2 -COOX , -CH 2 -NH 2, a -NH-alk, -NH-Ar, -NH 2 or -NH-Het, R 13 is alkyl or phenyl in and, R 30 is -NH-alk, -NH-Ar, or an -NH 2 or -NH-Het, or R is 2-imidazolylmethyl group and each of R 1 and R 2 are a hydrogen atom Yes] compound. The compounds of formula (I) are α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, also known as quisqualate receptors. Furthermore, the compounds of formula (I) are non-competitive N-methyl aspartate (NMDA) receptor antagonists, and in particular NMDA receptor glycine regulatory site ligands. |