Solution-Phase Parallel Synthesis and SAR of Homopiperazinyl Analogs as Positive Allosteric Modulators of mGlu4

被引:5
作者
Cheung, Yiu-Yin [1 ,2 ,3 ]
Zamorano, Rocio [1 ,2 ]
Blobaum, Anna L. [1 ,2 ]
Weaver, C. David [1 ,2 ]
Conn, P. Jeffrey [1 ,2 ,5 ]
Lindsley, Craig W. [1 ,2 ,3 ,4 ,5 ]
Niswender, Colleen M. [1 ,2 ]
Hopkins, Corey R. [1 ,2 ,3 ,4 ]
机构
[1] Vanderbilt Univ, Med Ctr, Dept Pharmacol, Nashville, TN 37232 USA
[2] Vanderbilt Univ, Med Ctr, Vanderbilt Program Drug Discovery, Nashville, TN 37232 USA
[3] Vanderbilt Specialized Chem Ctr Accelerated Probe, Nashville, TN 37232 USA
[4] Vanderbilt Univ, Dept Chem, Nashville, TN 37232 USA
[5] Vanderbilt Univ, Vanderbilt Inst Chem Biol, Nashville, TN 37232 USA
关键词
metabotropic glutamate receptor 4; mGlu(4); structure-activity relationship; parallel synthesis; GLUTAMATE-RECEPTOR; 4; PARKINSONS-DISEASE; MGLUR4; DISCOVERY; PAMS;
D O I
10.1021/co1000508
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
Using a functional high-throughput screening (HTS) and subsequent solution-phase parallel synthesis approach, we have discovered a novel series of positive allosteric modulators for mGlu(4), a G-protein coupled receptor. This series is comprised of a homopiperazine central core. The solution-phase parallel synthesis and SAP, of analogs derived from this series will be presented. This series of positive allosteric modulators of mGlu(4) provide critical research tools to further probe the mGlu(4)-mediated effects in Parkinson's disease.
引用
收藏
页码:159 / 165
页数:7
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