Structure-activity relationships of substituted 5H-thiazolo [3,2-a]pyrimidines as group 2 metabotropic glutamate receptor antagonists

Citation
J. Wichmann et al., Structure-activity relationships of substituted 5H-thiazolo [3,2-a]pyrimidines as group 2 metabotropic glutamate receptor antagonists, BIOORG MED, 9(11), 1999, pp. 1573-1576
Citations number
12
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
11
Year of publication
1999
Pages
1573 - 1576
Database
ISI
SICI code
0960-894X(19990607)9:11<1573:SROS5[>2.0.ZU;2-G
Abstract
A series of 5H-thiazolo[3,2-a]pyrimidine derivatives 1 was studied with res pect to the inhibition of 1S,3R-ACPD (10 mu M)-stimulated GTP gamma(35)S bi nding on rat mGlu2 receptor transfected cell membranes. The influence of su bstituents at position 6 and 7 as well as the substitution pattern of the t wo phenyl-rings in position 2 and 5 on the activity is discussed. (C) 1999 Elsevier Science Ltd. All rights reserved.