Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)
Research output: Contribution to journal › Journal article › Research › peer-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.
|Journal||Bioorganic & Medicinal Chemistry Letters|
|Number of pages||4|
|Publication status||Published - 1 Sep 2010|
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