2. Academic Validation
  3. Α-amino-β-fluorocyclopropanecarboxylic acids as a new tool for drug development: synthesis of glutamic acid analogs and agonist activity towards metabotropic glutamate receptor 4

Α-amino-β-fluorocyclopropanecarboxylic acids as a new tool for drug development: synthesis of glutamic acid analogs and agonist activity towards metabotropic glutamate receptor 4

  • Bioorg Med Chem. 2012 Aug 1;20(15):4716-26. doi: 10.1016/j.bmc.2012.06.006.
Gérald Lemonnier 1,  Cédric Lion,  Jean-Charles Quirion,  Jean-Philippe Pin,  Cyril Goudet,  Philippe Jubault
Affiliations

Affiliation

  • 1 INSA de Rouen and Université de Rouen, CNRS, UMR 6014 & FR 3038, COBRA, IRCOF, 1 rue Tesnière, 76821 Mont-Saint-Aignan Cedex, France.
PMID: 22750138 DOI: 10.1016/j.bmc.2012.06.006
Abstract

Herein we describe the diastereoselective synthesis of glutamic acid analogs and the evaluation of their agonist activity towards metabotropic glutamate receptor subtype 4 (mGluR4). These analogs are based on a monofluorinated cyclopropane core substituted with an α-aminoacid function. The potential of this new building block as a tool for the development of a novel class of drugs is demonstrated with racemic analog 11a that displayed the best agonist activity with an EC50 of 340 nM.

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