title: Structure-activity relationships of substituted 5H-thiazolo[3,2-a]pyrimidines as group 2 metabotropic glutamate receptor antagonists.
abstract: 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.
authors.affiliation: Pharma Division, Preclinical CNS Research, F. Hoffmann-La Roche Ltd., Basel. juergen.wichmann@roche.com
authors.forename: J
authors.initials: J
authors.lastname: Wichmann
authors.forename: G
authors.initials: G
authors.lastname: Adam
authors.forename: S
authors.initials: S
authors.lastname: Kolczewski
authors.forename: V
authors.initials: V
authors.lastname: Mutel
authors.forename: T
authors.initials: T
authors.lastname: Woltering
mesh_terms: 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
chemical_list: D018691:Excitatory Amino Acid Antagonists; D011743:Pyrimidines