168045-73-6Relevant articles and documents
Pyrrolylquinoxalinediones: A new class of AMPA receptor antagonists
Lubisch,Behl,Hofmann
, p. 2887 - 2892 (1996)
Pyrrolylquinoxalinediones were synthesized and their affinities for the AMPA receptor were determined. Most compounds showed moderate to good affinities. The acetic acid derivative 8b exhibited a K(i) value of 70 nM and was equipotent to NBQX 1. Structure activity relationships are discussed. Selected compounds were tested for their potency to inhibit AMPA induced lethal convulsions in mice. In this in vivo model the compounds showed improved potency compared with NBQX.
2,3(1H,4H)quinoxalinedione
-
, (2008/06/13)
2,3(1H,4H)-quinoxalinediones of the formula I STR1 where R1 is hydrogen, an aliphatic radical which has up to 12 carbons and can be substituted by one of the following: phenyl, cyclopentyl, cyclohexyl or --CO--R3, --CO--O--R3 or --CO--NH--R3, where R3 is hydrogen, C1 -C4 -alkyl, phenyl, benzyl or 1-phenylethyl, a cycloaliphatic radical with up to 12 carbons or phenyl, where the cyclic groups in R1 can have up to three of the following substituents: C1 -C4 -alkyl, C1 -C4 -haloalkyl, C1 -C4 -alkoxy, C1 -C4 -haloalkoxy, halogen, nitro, cyano, --CO--O--R3 and --CO--NH--R3 ; R2 is 1-pyrrolyl which can have up to two of the following substituents: C1 -C4 -alkyl, phenyl, phenylsulfonyl, nitro, cyano and --CO--O--R3, --CO--NH--R3, --CH2 --O--R3, --O--R3 and --CH=NO--R3 R radicals are identical or different and are the following: C1 -C4 -alkyl, C1 -C4 -alkoxy, trifluoromethyl, trichloromethyl, trifluoromethoxy, trichloromethoxy, fluorine, chlorine, bromine, iodine, nitro, cyano and --CO--O--R3 and --CO--NH--R3 as well as a fused-on benzene ring; n is 0-3, and 2,3(1H,4H)-quinoxalinediones I' STR2 where R1 has the stated meanings, are suitable as drugs in the treatment of neurodegenerative disorders and neurotoxic disturbances of the central nervous system.
