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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 12期

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 [J].

BIRCH, PJ ;

GROSSMAN, CJ ;

HAYES, AG .

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 [J].

COLLINGRIDGE, GL ;

SINGER, W .

TRENDS IN PHARMACOLOGICAL SCIENCES, 1990, 11 (07) :290-296

[4] ANTICONVULSANT ACTION OF EXCITATORY AMINO-ACID ANTAGONISTS [J].

CROUCHER, MJ ;

COLLINS, JF ;

MELDRUM, BS .

SCIENCE, 1982, 216 (4548) :899-901

[5] CONVENIENT PROCEDURE FOR THE PREPARATION OF ALKYL AND ARYL SUBSTITUTED N-(AMINOALKYLACYL)SULFONAMIDES [J].

DRUMMOND, JT ;

JOHNSON, G .

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 [J].

DUNCIA, JV ;

PIERCE, ME ;

SANTELLA, JB .

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 [J].

FRANDSEN, A ;

DREJER, J ;

SCHOUSBOE, A .

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 [J].

GRAY, NM ;

DAPPEN, MS ;

CHENG, BK ;

CORDI, AA ;

BIESTERFELDT, JP ;

HOOD, WF ;

MONAHAN, JB .

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 [J].

HONORE, T ;

DAVIES, SN ;

DREJER, J ;

FLETCHER, EJ ;

JACOBSEN, P ;

LODGE, D ;

NIELSEN, FE .

SCIENCE, 1988, 241 (4866) :701-703