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

Engers DW, Gentry PR, Williams R, Bolinger JD, Weaver CD, Menon UN, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR
Bioorg Med Chem Lett. 2010 20 (17): 5175-8

PMID: 20667732 · PMCID: PMC2922490 · DOI:10.1016/j.bmcl.2010.07.007

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.

Copyright 2010 Elsevier Ltd. All rights reserved.

MeSH Terms (5)

Allosteric Regulation Aniline Compounds Receptors, Metabotropic Glutamate Structure-Activity Relationship Sulfonamides

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