Structure-activity relationships of substituted 5H-thiazolo[3,2-a]pyrimidines as group 2 metabotropic glutamate receptor antagonists.
A series of 5H-thiazolo[3,2-a]pyrimidine derivatives 1 was studied with respect to the inhibition of 1S,3R-ACPD (10 microM)-stimulated GTP gamma35S binding on rat mGlu2 receptor transfected cell membranes. The influence of substituents at position 6 and 7 as well as the substitution pattern of the two phenyl-rings in position 2 and 5 on the activity is discussed.
Wichmann
J
J
Pharma Division, Preclinical CNS Research, F. Hoffmann-La Roche Ltd., Basel. juergen.wichmann@roche.com
Adam
G
G
Kolczewski
S
S
Mutel
V
V
Woltering
T
T
D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D018691:Excitatory Amino Acid Antagonists / Q000737:chemistry*; D007700:Kinetics; D008956:Models, Chemical; D011743:Pyrimidines / Q000737:chemistry*; D051381:Rats; D013329:Structure-Activity Relationship
D018691:Excitatory Amino Acid Antagonists; D011743:Pyrimidines