PYRROLYLQUINOXALINEDIONES - THE IMPORTANCE OF PYRROLIC SUBSTITUTION ON AMPA RECEPTOR-BINDING

Authors
LUBISCH W BEHL B HOFMANN HP
Citation
W. Lubisch et al., PYRROLYLQUINOXALINEDIONES - THE IMPORTANCE OF PYRROLIC SUBSTITUTION ON AMPA RECEPTOR-BINDING, Bioorganic & medicinal chemistry letters, 7(9), 1997, pp. 1101-1106
Citations number
24
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
9
Year of publication
1997
Pages
1101 - 1106
Database
ISI
SICI code
0960-894X(1997)7:9<1101:P-TIOP>2.0.ZU;2-5
Abstract
Pyrrolylquinoxalinediones were synthesized to elucidate the value of p yrrolic substitution pattern on AMPA receptor binding. We discovered t hat amide and urea residues at the 3'-position at pyrrol ring favor af finity to AMPA receptor. Particularly, the phenylurea 13n exhibited a K-i value of 4 nM in AMPA receptor binding and represents the most pot ent competitive AMPA antagonist reported to dare. (C) 1997 Elsevier Sc ience Ltd.