Design, synthesis and preliminary evaluation of novel 3′-Substituted carboxycyclopropylglycines as antagonists at group 2 metabotropic glutamate receptors

…, G Costantino, M Marinozzi, A Macchiarulo…

Index: Pellicciari, Roberto; Costantino, Gabriele; Marinozzi, Maura; Macchiarulo, Antonio; Amori, Laura; Josef Flor, Peter; Gasparini, Fabrizio; Kuhn, Rainer; Urwyler, Stephan Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 24 p. 3179 - 3182

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Citation Number: 25

Abstract

Two novel 3′-substituted carboxycylopropylglycines,(2S, 1′ S, 2′ S, 3′ R)-2-(3′- xanthenylmethyl-2′-carboxycyclopropyl) glycine (8a) and (2S, 1′ S, 2′ S, 3′ R)-2-(3′- xanthenylethyl-2′-carboxycyclopropyl) glycine (8b), were synthesized and evaluated as mGluR ligands. Compound 8b showed to be a potent group II antagonist with submicromolar activity.