Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

Research output: Contribution to journalJournal articleResearchpeer-review

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

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.

Original languageEnglish
JournalBioorganic & Medicinal Chemistry Letters
Volume20
Issue number17
Pages (from-to)5175-8
Number of pages4
ISSN0960-894X
DOIs
Publication statusPublished - 1 Sep 2010
Externally publishedYes

Bibliographical note

Copyright 2010 Elsevier Ltd. All rights reserved.

    Research areas

  • Allosteric Regulation, Aniline Compounds/chemical synthesis, Receptors, Metabotropic Glutamate/drug effects, Structure-Activity Relationship, Sulfonamides/chemical synthesis

ID: 213625970