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Synthesis and preliminary pharmacological evaluation of the four stereoisomers of (2S)-2-(2'-phosphono-3'-phenylcyclopropyl)glycine, the first class of 3'-substituted trans C1'-2'-2-(2'-phosphonocyclopropyl)glycines |
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| Authors: | Marinozzi Maura Serpi Michaela Amori Laura Gavilan Diaz Monica Costantino Gabriele Meyer Udo Flor Peter J Gasparini Fabrizio Heckendorn Roland Kuhn Rainer Giorgi Gianluca Hermit Mette Brunsgaard Thomsen Christian Pellicciari Roberto |
| Affiliation: | Dipartimento di Chimica e Tecnologia del Farmaco, Università di Perugia, Via del Liceo, 1- I-06123 Perugia, Italy. |
| Abstract: | Four stereoisomers of (2S)-2-(2'-phosphono-3'-phenylcyclopropyl)glycine were synthesized by a stereocontrolled synthetic procedure and evaluated as mGluRs ligands. The (2S,1'R,2'S,3'R)-isomer (PPCG-2) showed to be a group III mGluRs selective ligand endowed with a moderate potency as mGluR4/mGluR6 agonist. |
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