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

D.W. Engers, P.R. Gentry, Richard Williams, J.D. Bolinger, C.D. Weaver, Aric Menon, Lorna Conn, C.W. Lindsley, C.M. Niswender, Fiona Hopkins

Research output: Contribution to journalArticle

20 Citations (Scopus)

Abstract

Herein we disclose the synthesis and SAR of a series of 4-(phenylsulfamoyl)phenylacetamide compounds as mGlu(4) 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) mGlu(4) PAM reported to date. (C) 2010 Elsevier Ltd. All rights reserved.
Original languageEnglish
Pages (from-to)5175-5178
Number of pages4
JournalBioorganic & Medicinal Chemistry Letters
Volume20
Issue number17
DOIs
Publication statusPublished - 01 Sep 2010

ASJC Scopus subject areas

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

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