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Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGlu?.

ABSTRACT: 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?, a G-protein coupled receptor. This series is comprised of a homopiperazine central core. The solution-phase parallel synthesis and SAR of analogs derived from this series will be presented. This series of positive allosteric modulators of mGlu? provide critical research tools to further probe the mGlu?-mediated effects in Parkinson's disease.

SUBMITTER: Cheung YY

PROVIDER: S-EPMC3057427 | biostudies-literature | 2011 Mar

REPOSITORIES: biostudies-literature

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Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGlu₄.

Cheung Yiu-Yin YY Zamorano Rocio R Blobaum Anna L AL Weaver C David CD Conn P Jeffrey PJ Lindsley Craig W CW Niswender Colleen M CM Hopkins Corey R CR

ACS combinatorial science 20110221 2

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 mGlu₄, a G-protein coupled receptor. This series is comprised of a homopiperazine central core. The solution-phase parallel synthesis and SAR of analogs derived from this series will be presented. This series of positive allosteric modulators of mGlu₄ provide critical research tools to further probe the mGlu₄-mediate ...[more]

PMID: 21338051

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