Synthesis and inhibitory activities at mGluRs of 3-alkylated and N-alkylated cyclopentyl-glutamate analogues

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Journal Article
Tetrahedron, 2013, 69 (12), pp. 2577 - 2587
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The conformationally restricted glutamate analogues, 3-alkyl-1-amino-2- cyclopentene-1,3-dicarboxylates and N-alkylated analogues have been prepared in a regioselective and diastereoselective manner. From the biological studies of the 3-alkylated analogues, compound 13b was found to be the most potent antagonist (IC50 7.7 μM) at mGluR2. Amongst the N-alkylated analogues, compound 20 was found to be a partial agonist (EC50 9.5 μM) and as well as an antagonist (IC50 47 μM) at mGluR2. © 2013 Elsevier Ltd. All rights reserved.
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