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ID: ALA1147898

Journal: Bioorg Med Chem

Title: 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.

Authors: Marinozzi M, Serpi M, Amori L, Gavilan Diaz M, Costantino G, Meyer U, Flor PJ, Gasparini F, Heckendorn R, Kuhn R, Giorgi G, Hermit MB, Thomsen C, Pellicciari R.

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.

CiteXplore: 17350267

DOI: 10.1016/j.bmc.2007.02.040