SYNTHESIS AND GLUTAMATE ANTAGONIST ACTIVITY OF 4-PHOSPHONOALKYLQUINOLINE DERIVATIVES - A NOVEL CLASS OF NON-NMDA ANTAGONIST
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
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
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.