Title of article :
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 Original Research Article
Author/Authors :
Maura Marinozzi، نويسنده , , Michaela Serpi، نويسنده , , Laura Amori، نويسنده , , Monica Gavilan Diaz، نويسنده , , Gabriele Costantino، نويسنده , , Bernd Günther and Udo Meyer، نويسنده , , Peter J. Flor، نويسنده , , Fabrizio Gasparini، نويسنده , , Roland Heckendorn، نويسنده , , Rainer Kuhn، نويسنده , , Gianluca Giorgi، نويسنده , , Mette Brunsgaard Hermit، نويسنده , , Christian Thomsen، نويسنده , , Roberto Pellicciari، نويسنده ,
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.
Keywords :
3?-Substituted-2-(2?-phosphonocyclopropyl)glycines , metabotropic glutamate receptors , Conformationally constrained amino acids
