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 (10μM)-stimulated GTP γ 35S 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 pheny...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1999-06, Vol.9 (11), p.1573-1576
Main Authors: Wichmann, Jürgen, Adam, Geo, Kolczewski, Sabine, Mutel, Vincent, Woltering, Thomas
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
CHO Cells
Cricetinae
Excitatory Amino Acid Antagonists - chemistry
Glutamatergic system (aspartate and other excitatory aminoacids)
Kinetics
Medical sciences
Models, Chemical
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Pyrimidines - chemistry
Rats
Structure-Activity Relationship
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Summary:A series of 5H-thiazolo[3,2-a]pyrimidine derivatives 1 was studied with respect to the inhibition of 1S,3R-ACPD (10μM)-stimulated GTP γ 35S 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. A series of 5H-thiazolo[3,2-a]pyrimidine derivatives was studied with respect to the inhibition of 1S,2R-ACPD (10μM)-stimulated GTP γ 35S binding on rat mGluR2 transfected cell membranes. The influence of substituents at position 6 (R 2) and 7 (R 1) as well as the substitution pattern of the two phenyl-rings (R 3, R 4) on the activity is discussed.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00227-9