PYRROLYLQUINOXALINEDIONES - DICARBOXYLATES AS HIGHLY POTENT AMPA RECEPTOR ANTAGONISTS

Authors
LUBISCH W BEHL B HOFMANN HP TESCHENDORF HJ
Citation
W. Lubisch et al., PYRROLYLQUINOXALINEDIONES - DICARBOXYLATES AS HIGHLY POTENT AMPA RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 7(19), 1997, pp. 2441-2446
Citations number
32
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
19
Year of publication
1997
Pages
2441 - 2446
Database
ISI
SICI code
0960-894X(1997)7:19<2441:P-DAHP>2.0.ZU;2-9
Abstract
Pyrrolylquinoxalinediones carrying carboxylates at the pyrrole side-ch ain were synthesized and evaluated for AMPA receptor binding and for s electivity over other glutamate receptors. Particularly dicarboxy deri vatives represent selective and highly potent AMPA antagonists. Moreov er, several compounds displayed a remarkable efficacy against AMPA ind uced lethal convulsions and maximal electroshock seizures (MES) in mic e. The good in vivo efficacy of the highly polar compounds suggests th e involvement of an active transport mechanism. (C) 1997 Elsevier Scie nce Ltd.