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

  • Bioorg Med Chem Lett. 2006 Jan 1;16(1):196-9. doi: 10.1016/j.bmcl.2005.09.014.
Laura Amori  1 ,  Michaela Serpi ,  Maura Marinozzi ,  Gabriele Costantino ,  Monica Gavilan Diaz ,  Mette Brunsgaard Hermit ,  Christian Thomsen ,  Roberto Pellicciari
Affiliations
  • 1. Dipartimento di Chimica e Tecnologia del Farmaco, Università di Perugia, Via del Liceo, 1-06123 Perugia, Italy.
PMID: 16213710 DOI: 10.1016/j.bmcl.2005.09.014
Abstract

Two novel constrained l-AP4 analogues, (2S,1'R,2'S)- and (2S,1'S,2'R)-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.