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
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
Journal title :
Tetrahedron
