N-Phosphonoalkyl-5-aminomethylquinoxaline-2,3-diones:: in vivo active AMPA and NMDA(glycine) antagonists.

被引:31
作者
Auberson, YP [1 ]
Acklin, P [1 ]
Bischoff, S [1 ]
Moretti, R [1 ]
Ofner, S [1 ]
Schmutz, M [1 ]
Veenstra, SJ [1 ]
机构
[1] Novartis Pharma AG, CH-4002 Basel, Switzerland
关键词
D O I
10.1016/S0960-894X(98)00720-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
N-Substituted 5-aminomethylquinoxalinediones containing carboxy or phosphonic acids yield potent and selective AMPA and/or NMDA (glycine-binding site) antagonists. Phosphonic acid derivatives are particularly water-soluble and display potent anticonvulsant effects in the electroshock-induced convulsion assay in mice. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:249 / 254
页数:6
相关论文
共 25 条
[1]   5-aminomethylquinoxaline-2,3-diones, Part III: Arylamide derivatives as highly potent and selective glycine-site NMDA receptor antagonists [J].
Acklin, P ;
Allgeier, H ;
Auberson, YP ;
Bischoff, S ;
Ofner, S ;
Sauer, D ;
Schmutz, M .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (05) :493-498
[2]   5-Aminomethylquinoxaline-2,3-diones. Part II: N-aryl derivatives as novel NMDA/glycine and AMPA antagonists. [J].
Auberson, YP ;
Acklin, P ;
Allgeier, H ;
Biollaz, M ;
Bischoff, S ;
Ofner, S ;
Veenstra, SJ .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (01) :71-74
[3]   5-Aminomethylquinoxaline-2,3-diones. Part I: A novel class of AMPA receptor antagonists. [J].
Auberson, YP ;
Bischoff, S ;
Moretti, R ;
Schmutz, M ;
Veenstra, SJ .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (01) :65-70
[4]  
BIGGE FC, 1995, J MED CHEM, V38, P3270
[5]   Glutamate, GABA and epilepsy [J].
Bradford, HF .
PROGRESS IN NEUROBIOLOGY, 1995, 47 (06) :477-511
[6]  
CHOI DW, 1990, ANNU REV NEUROSCI, V13, P171, DOI 10.1146/annurev.neuro.13.1.171
[7]   Glutamate antagonists for Parkinson's disease - Rationale for use and therapeutic implications [J].
Cooper, AJ ;
Carroll, CB ;
Mitchell, IJ .
CNS DRUGS, 1998, 9 (06) :421-429
[8]   Applications of simulated moving-bed chromatography to the separation of the enantiomers of chiral drugs [J].
Francotte, ER ;
Richert, P .
JOURNAL OF CHROMATOGRAPHY A, 1997, 769 (01) :101-107
[9]   THE BINDING OF [AMPA-H-3, A STRUCTURAL ANALOG OF GLUTAMIC-ACID, TO RAT-BRAIN MEMBRANES [J].
HONORE, T ;
LAURIDSEN, J ;
KROGSGAARDLARSEN, P .
JOURNAL OF NEUROCHEMISTRY, 1982, 38 (01) :173-178
[10]  
Loschmann PA, 1997, SYNAPSE, V26, P381, DOI 10.1002/(SICI)1098-2396(199708)26:4<381::AID-SYN6>3.0.CO