Synthesis and antagonist activities of 4-aryl-substituted conformationally restricted cyclopentenyl and cyclopentanyl-glutamate analogues

The conformationally restricted glutamate analogues, 4-aryl-1-amino-2-cyclopentene-1,3-dicarboxylates and their cyclopentane analogues have been prepared in a diastereoselective manner. Biological studies of 12a and 12b indicates that both compounds are modest antagonists at mGluR2. Graphical abstra...

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Bibliographic Details
Published in:Tetrahedron 2005-02, Vol.61 (7), p.1803-1812
Main Authors: Ung, Alison T., Pyne, Stephen G., Batenburg-Nguyen, Uta, Davis, Andrew S., Sherif, Azlifa, Bischoff, François, Lesage, Anne S.J.
Format: Article
Language:English
Subjects:
Antagonists
Heck reaction
Metabotropic glutamate receptors
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Summary:The conformationally restricted glutamate analogues, 4-aryl-1-amino-2-cyclopentene-1,3-dicarboxylates and their cyclopentane analogues have been prepared in a diastereoselective manner. Biological studies of 12a and 12b indicates that both compounds are modest antagonists at mGluR2. Graphical abstract
ISSN:0040-4020
1464-5416
DOI:10.1016/j.tet.2004.12.024