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

通过功能性高通量筛选 (HTS) 鉴定的新型 4-(苯磺酰基)苯乙酰胺 mGlu4 正变构调节剂 (PAM) 的合成和构效关系研究

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作者：Engers,Darren W,Gentry,Patrick R,Williams,Richard,Bolinger,Julie D,Weaver,C David,Menon,Usha N,Conn,P Jeffrey,Lindsley,Craig W,Niswender,Colleen M,Hopkins,Corey R
期刊：Bioorganic & Medicinal Chemistry Letters影响因子：2.200
时间：2010起止号：2010 Sep 1;20(17):5175-8
doi：10.1016/j.bmcl.2010.07.007

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.

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