173156-22-4Relevant academic research and scientific papers
Imidazo?1,2-A! pyrazine-4-one, preparation thereof and drugs containing same
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, (2008/06/13)
Compounds of formula (1) STR1 wherein either R is C=R3, C(R4)R5 or CH--R6, R1 and R2 are hydrogen, halogen, alkyl, alkoxy, amino, acylamino, --NH--CO--NH--Ar, --N=CH--N(alk)alk', nitro, cyano, phenyl, imidazolyl or SO3 H, R3 is oxygen, NOH, NO-alk-COOK or CH--R7, R4 is alkyl, -alk-Het or alk-Ar, R5 is alkyl, -alk-Het or -alk-Ar, or C(R4)R5 is cycloalkyl, R6 is hydroxy, alkyl, NR8 R9, -alk-OH, -alk-NR8 R9, -alk-Ar or -alk-Het, R7 is hydroxy, alkyl, phenyl, -alk-Ar, -alk-Het, NR10 R11 or a heterocyclic ring, R8 and R9 are alkyl, or R8 is hydrogen and R9 is hydrogen or alkyl, --COR12, --CSR30 or --SO2 R13, R10 and R11 are alkyl or cycloalkyl, R12 is alkyl, cycloalkyl, phenyl, --COO-alk, --CH2 --COOX, --CH2 NH2, --NH-alk, --NH--Ar, --NH2 or --NH-Het, R13 is alkyl or phenyl, R30 is --NH-alk, --NH--Ar, --NH2 or --NH-Het, R13 is alkyl or phenyl, R30 is --NH-alk, --NH--Ar, --NH2 or --NH-Het; or R is a 2-imidazolylmethyl radical and each of R1 and R2 is a hydrogen atom. The compounds of formula (I) are α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, said receptor also being known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists, and especially NMDA receptor gylcine modulation site ligands.
