Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 20, Issue 15, Pages 4716-4726Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.06.006
Keywords
Metabotropic glutamate receptor; Fluorine; Amino-acids; Cyclopropane; Phosphonic acid
Funding
- MESR (Ministere de l'Enseignement Superieur et de la Recherche)
- Region Haute-Normandie (CRUNCH program)
- INSA of Rouen
- OSEO-ANVAR [A0702006 P]
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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 alpha-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. (C) 2012 Elsevier Ltd. All rights reserved.
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