SYNTHESIS AND EXCITATORY AMINO-ACID PHARMACOLOGY OF SOME NOVEL QUINOXALINEDIONES

被引:28
作者
EPPERSON, JR
HEWAWASAM, P
MEANWELL, NA
BOISSARD, CG
GRIBKOFF, VK
POSTMUNSON, D
机构
[1] Bristol-Myers Squibb, Pharmaceutical Research Institute, Wallingford, CT 06492
关键词
D O I
10.1016/S0960-894X(01)80768-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and amino acid pharmacology of twelve N-substituted quinoxalinediones is reported. In particular, compounds 4a and 4b show significant antagonism at both the AMPA and glycine-site NMDA receptors. The functional antagonism of 4a has been demonstrated.
引用
收藏
页码:2801 / 2804
页数:4
相关论文
共 24 条
  • [1] 6,7-DINITRO-QUINOXALINE-2,3-DION AND 6-NITRO,7-CYANO-QUINOXALINE-2,3-DION ANTAGONIZE RESPONSES TO NMDA IN THE RAT SPINAL-CORD VIA AN ACTION AT THE STRYCHNINE-INSENSITIVE GLYCINE RECEPTOR
    BIRCH, PJ
    GROSSMAN, CJ
    HAYES, AG
    [J]. EUROPEAN JOURNAL OF PHARMACOLOGY, 1988, 156 (01) : 177 - 180
  • [2] CARTER A J, 1992, Drugs of the Future, V17, P595
  • [3] EXCITATORY AMINO-ACID RECEPTORS AND SYNAPTIC PLASTICITY
    COLLINGRIDGE, GL
    SINGER, W
    [J]. TRENDS IN PHARMACOLOGICAL SCIENCES, 1990, 11 (07) : 290 - 296
  • [4] ANTICONVULSANT ACTION OF EXCITATORY AMINO-ACID ANTAGONISTS
    CROUCHER, MJ
    COLLINS, JF
    MELDRUM, BS
    [J]. SCIENCE, 1982, 216 (4548) : 899 - 901
  • [5] CONVENIENT PROCEDURE FOR THE PREPARATION OF ALKYL AND ARYL SUBSTITUTED N-(AMINOALKYLACYL)SULFONAMIDES
    DRUMMOND, JT
    JOHNSON, G
    [J]. TETRAHEDRON LETTERS, 1988, 29 (14) : 1653 - 1656
  • [6] 3 SYNTHETIC ROUTES TO A STERICALLY HINDERED TETRAZOLE - A NEW ONE-STEP MILD CONVERSION OF AN AMIDE INTO A TETRAZOLE
    DUNCIA, JV
    PIERCE, ME
    SANTELLA, JB
    [J]. JOURNAL OF ORGANIC CHEMISTRY, 1991, 56 (07) : 2395 - 2400
  • [7] DIRECT EVIDENCE THAT EXCITOTOXICITY IN CULTURED NEURONS IS MEDIATED VIA N-METHYL-D-ASPARTATE (NMDA) AS WELL AS NON-NMDA RECEPTORS
    FRANDSEN, A
    DREJER, J
    SCHOUSBOE, A
    [J]. JOURNAL OF NEUROCHEMISTRY, 1989, 53 (01) : 297 - 299
  • [8] NOVEL INDOLE-2-CARBOXYLATES AS LIGANDS FOR THE STRYCHNINE-INSENSITIVE N-METHYL-D-ASPARTATE-LINKED GLYCINE RECEPTOR
    GRAY, NM
    DAPPEN, MS
    CHENG, BK
    CORDI, AA
    BIESTERFELDT, JP
    HOOD, WF
    MONAHAN, JB
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (04) : 1283 - 1292
  • [9] GRIBKOFF VK, 1983, J PHYSL, V334, P33
  • [10] QUINOXALINEDIONES - POTENT COMPETITIVE NON-NMDA GLUTAMATE RECEPTOR ANTAGONISTS
    HONORE, T
    DAVIES, SN
    DREJER, J
    FLETCHER, EJ
    JACOBSEN, P
    LODGE, D
    NIELSEN, FE
    [J]. SCIENCE, 1988, 241 (4866) : 701 - 703