Synthesis and preliminary pharmacological evaluation of the four stereoisomers of (2S)-2-(2' -phosphono -3'-phenylcyclopropyl)glycine, the first class of 3'-substituted transc1' - 2'-2-(2 '-phosphonocyclopropyl)glycines

Abstract Four stereoisomers of (2 S )-2-(2′-phosphono-3′-phenylcyclopropyl)glycine were synthesized by a stereocontrolled synthetic procedure and evaluated as mGluRs ligands. The (2 S ,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.