Synthesis of heterocyclic enol ethers and their use as group 2 metabotropic glutamate receptor antagonists.
Heterocyclic enol ethers of type 1 were studied with respect to the inhibition of 1S,3R-ACPD (10 microM)-stimulated GTP gamma35S binding on rat mGluR2 transfected cell membranes. The structure activity relationship with regard to the substitution pattern of the phenyl ring, the oxygen substituent and the nature of the heterocycle is discussed.
Kolczewski
S
S
Pharma Division, Preclinical CNS Research, F. Hoffmann-La Roche Ltd., Basel. sabine.kolczewski@roche.com
Adam
G
G
Stadler
H
H
Mutel
V
V
Wichmann
J
J
Woltering
T
T
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D004987:Ethers / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018691:Excitatory Amino Acid Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000378:metabolism; D051381:Rats; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013462:Sulfur Radioisotopes; D014162:Transfection
D004987:Ethers; D018691:Excitatory Amino Acid Antagonists; D018094:Receptors, Metabotropic Glutamate; D013462:Sulfur Radioisotopes; C108822:metabotropic glutamate receptor 2; D016244:Guanosine 5'-O-(3-Thiotriphosphate)