Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS).
AUTHORS
Engers
DWDarren W ,
Gentry
PR Patrick R ,
Williams
R Richard ,
Bolinger
JD Julie D ,
Weaver
CD C David ,
Menon
UN Usha N ,
Conn
PJ P Jeffrey ,
Lindsley
CW Craig W ,
Niswender
CM Colleen M ,
Hopkins
CR Corey R .
Bioorganic & medicinal chemistry letters. 2010 9 1; 20(17).
5175-8
- PMID: 20667732[PubMed].
- PMCID: PMC2922490.
- NIHMSID: NIHMS221889
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.
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.