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Design, synthesis and preliminary evaluation of novel 3′-Substituted carboxycyclopropylglycines as antagonists at group 2 metabotropic glutamate receptors |
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| Authors: | Roberto Pellicciari Gabriele Costantino Maura Marinozzi Antonio Macchiarulo Laura Amori Peter Josef Flor Fabrizio Gasparini Rainer Kuhn Stephan Urwyler |
| Institution: | a Dipartimento di Chimica e Tecnologia del Farmaco, Università di Perugia, Via del Liceo 1, 06127, Perugia, Italy b Novartis Pharma AG, Nervous System Research, Basel, Switzerland |
| 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. |
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