Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs)

Darren W. Engers, Colleen M. Niswender, C. David Weaver, Satyawan Jadhav, Usha N. Menon, Rocio Zamorano, P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins

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Abstract

We report the synthesis and evaluation of a series of heterobiaryl amides as positive allosteric modulators of mGluR4. Compounds 9b and 9c showed submicromolar potency at both human and rat mGluR4. In addition, both 9b and 9c were shown to be centrally penetrant in rats using nontoxic vehicles, a major advance for the mGluR4 field.

Original languageEnglish (US)
Pages (from-to)4115-4118
Number of pages4
JournalJournal of Medicinal Chemistry
Volume52
Issue number14
DOIs
StatePublished - Jul 23 2009

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ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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