Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu 4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

Darren W. Engers, Patrick R. Gentry, Richard Williams, Julie D. Bolinger, C. David Weaver, Usha N. Menon, P. Jeffrey Conn, Craig W. Lindsley, Colleen M. Niswender, Corey R. Hopkins

Research output: Contribution to journalArticle

20 Scopus citations

Abstract

Herein we disclose the synthesis and SAR of a series of 4-(phenylsulfamoyl)phenylacetamide compounds as mGlu4 positive allosteric modulators (PAMs) that were identified via a functional HTS. An iterative parallel approach to these compounds culminated in the discovery of VU0364439 (11) which represents the most potent (19.8 nM) mGlu4 PAM reported to date.

Original languageEnglish (US)
Pages (from-to)5175-5178
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number17
DOIs
StatePublished - Sep 1 2010

Keywords

  • Functional high-throughput screen (HTS)
  • Metabotropic glutamate receptor 4
  • mGlu

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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