SYNTHESIS AND GLUTAMATE ANTAGONIST ACTIVITY OF 4-PHOSPHONOALKYLQUINOLINE DERIVATIVES - A NOVEL CLASS OF NON-NMDA ANTAGONIST

Authors
HAMILTON GS BEDNAR D BOROSKY SA HUANG Z ZUBROWSKI R FERKANY JW KARBON EW
Citation
Gs. Hamilton et al., SYNTHESIS AND GLUTAMATE ANTAGONIST ACTIVITY OF 4-PHOSPHONOALKYLQUINOLINE DERIVATIVES - A NOVEL CLASS OF NON-NMDA ANTAGONIST, Bioorganic & medicinal chemistry letters, 4(16), 1994, pp. 2035-2040
Citations number
20
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
16
Year of publication
1994
Pages
2035 - 2040
Database
ISI
SICI code
0960-894X(1994)4:16<2035:SAGAAO>2.0.ZU;2-Z
Abstract
The synthesis of ten 4-phosphonoalkylquinoline derivatives and the eva luation of their glutamate antagonist activity is described. Several c ompounds demonstrate significant antagonism at both 6-cyano-7-nitroqui noxalin-2,3-dione (CNQX) binding sites and the glycine regulatory site of the NMDA receptor. These compounds have also been shown to act as functional antagonists of kainic acid in Xenopus oocytes.