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.