Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers

  • Bioorg Med Chem Lett. 2009 Mar 15;19(6):1666-9. doi: 10.1016/j.bmcl.2009.01.108.
Eric Vieira  1 ,  Jörg Huwyler ,  Synèse Jolidon ,  Frédéric Knoflach ,  Vincent Mutel ,  Jürgen Wichmann
Affiliations
  • 1. Pharma Division, Discovery Research, F. Hoffmann-La Roche Ltd, CH-4070 Basel, Switzerland.
PMID: 19233648 DOI: 10.1016/j.bmcl.2009.01.108
Abstract

Small molecule mGluR1 enhancers, which are 9H-xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl- and (2H-tetrazol-5-yl)-amides, have been previously reported. Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides with improved pharmacokinetic properties have been designed and synthesized as useful pharmacological tools for the study of the physiological roles mediated by mGlu1 receptors. The synthesis and the structure-activity relationship of this class of positive allosteric modulators of mGlu1 receptors will be discussed in detail.

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