Design, synthesis and preliminary evaluation of novel 3'-substituted carboxycyclopropylglycines as antagonists at group 2 metabotropic glutamate receptors

  • Bioorg Med Chem Lett. 2001 Dec 17;11(24):3179-82. doi: 10.1016/s0960-894x(01)00656-4.
R Pellicciari  1 ,  G Costantino ,  M Marinozzi ,  A Macchiarulo ,  L Amori ,  P Josef Flor ,  F Gasparini ,  R Kuhn ,  S Urwyler
Affiliations
  • 1. Dipartimento di Chimica e Tecnologia del Farmaco, Università di Perugia, Via del Liceo 1, 06127, Perugia, Italy. [email protected]
PMID: 11720869 DOI: 10.1016/s0960-894x(01)00656-4
Abstract

Two novel 3'-substituted carboxycylopropylglycines, (2S,1'S,2'S,3'R)-2-(3'-xanthenylmethyl-2'-carboxycyclopropyl)glycine (8a) and (2S,1'S,2'S,3'R)-2-(3'-xanthenylethyl-2'-carboxycyclopropyl)glycine (8b), were synthesized and evaluated as mGluR ligands. Compound 8b showed to be a potent group II antagonist with submicromolar activity.