2-Substituted (2 SR)-2-amino-2-((1 SR, 2 SR)-2-carboxycycloprop-1-yl) glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 2. …

…, JH Kennedy, RA Wright, BG Johnson…

Index: Ornstein, Paul L.; Bleisch, Thomas J.; Arnold, M. Brian; Kennedy, Joseph H.; Wright, Rebecca A.; Johnson, Bryan G.; Tizzano, Joseph P.; Helton, David R.; Kallman, Mary Jeanne; Schoepp, Darryle D.; Herin, Marc Journal of Medicinal Chemistry, 1998 , vol. 41, # 3 p. 358 - 378

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Citation Number: 86

Abstract

In this paper we describe the synthesis of a series of α-substituted analogues of the potent and selective group II metabotropic glutamate receptor (mGluR) agonist (1S, 1'S, 2'S)- carboxycyclopropylglycine (2, L-CCG 1). Incorporation of a substituent on the amino acid carbon converted the agonist 2 into an antagonist. All of the compounds were prepared and tested as a series of four isomers, ie, two racemic diastereomers. On the basis of the ...