Synthesis and biological evaluation of (2S)- and (2R)-2-(3'-phosphonobicyclo[1.1.1]pentyl)glycines as novel group III selective metabotropic glutamate receptor ligands |
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Authors: | Filosa Rosanna Marinozzi Maura Costantino Gabriele Hermit Mette Brunsgaard Thomsen Christian Pellicciari Roberto |
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Affiliation: | Dipartimento di Chimica e Tecnologia del Farmaco, Università di Perugia, Via del Liceo, 1- 06123 Perugia, Italy. |
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Abstract: | The synthesis of (2S)- and (2R)-2-(3'-phosphonobicyclo[1.1.1]pentyl)glycine isomers (10 and 11), characterized by the bioisosteric replacement of the distal carboxylic group of 2-(3'-carboxybicyclo[1.1.1]pent-1-yl)glycine by the phosphonate moiety, was accomplished by a stereoselective Ugi condensation. The two isomers were tested for their activity against an array of metabotropic glutamate receptors, and the S-isomer (10) turned out to be a moderately potent and selective mGluR4 agonist. |
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