Title of article
Synthesis and inhibitory activities at mGluRs of 3-alkylated and N-alkylated cyclopentyl-glutamate analogues
Author/Authors
Alison T. Ung، نويسنده , , Stephen G. Pyne، نويسنده , , François Bischoff، نويسنده , , Anne S.J. Lesage، نويسنده , , Brian W. Skelton، نويسنده , , Allan H. White، نويسنده ,
Issue Information
هفته نامه با شماره پیاپی سال 2013
Pages
11
From page
2577
To page
2587
Abstract
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.
Keywords
Cyclopentyl-glutamate analogues , mGluR2 , antagonists , crystal structures , Agonists
Journal title
Tetrahedron
Serial Year
2013
Journal title
Tetrahedron
Record number
1105590
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