Synthesis and preliminary biological evaluation of (2S,1 ' R,2 ' S)-and (2S,1S,2 ' R)-2-(2 '-phosphonocyclopropyl)glycines, two novel conformationally constrained L-AP4 analogues

Two novel constrained L-AP4 analogues, (2S,1'R,2'S)- and (2S,1'S,2R)-2-(2'-phosphonocyclopropyl)glycines (7) and (8), were synthesized and evaluated as mGluR ligands. Compound 7 showed to be a group III mGluRs agonist with micromolar activity. (c) 2005 Elsevier Ltd. All rights reserved.