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Synthesis and antagonist activities of 4-aryl-substituted conformationally restricted cyclopentenyl and cyclopentanyl-glutamate analogues
Authors:Alison T Ung  Stephen G Pyne  Azlifa Sherif  Anne SJ Lesage
Institution:a Department of Chemistry, University of Wollongong, Wollongong, NSW 2522, Australia
b CNS Discovery Research, Johnson and Johnson Pharmaceutical Research and Development a Division of Janssen Pharmaceutica N.V., Beerse, B-2340, Belgium
Abstract: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.
Keywords:Metabotropic glutamate receptors  Antagonists  Heck reaction
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