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Structure-activity relationships of substituted 5H-thiazolo[3,2-a]pyrimidines as group 2 metabotropic glutamate
J Wichmann1, G Adam, S Kolczewski
1Pharma Division, Preclinical CNS Research, F. Hoffmann-La Roche Ltd., Basel. juergen.wichmann@roche.com
Bioorganic & Medicinal Chemistry Letters
|July 1, 1999
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.