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

Yiu Yin Cheung, Rocio Zamorano, Anna L. Blobaum, C. David Weaver, P. Jeffrey Conn, Craig W. Lindsley, Colleen M. Niswender, Corey R. Hopkins

Research output: Contribution to journalArticle

4 Scopus citations

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 formGlu4, 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-mediated effects in Parkinson's disease.

Original languageEnglish (US)
Pages (from-to)159-165
Number of pages7
JournalACS Combinatorial Science
Volume13
Issue number2
DOIs
StatePublished - Mar 14 2011

Keywords

  • Metabotropic glutamate receptor 4
  • Parallel synthesis
  • Structure - Activity relationship
  • mGlu

ASJC Scopus subject areas

  • Chemistry(all)

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    Cheung, Y. Y., Zamorano, R., Blobaum, A. L., Weaver, C. D., Conn, P. J., Lindsley, C. W., Niswender, C. M., & Hopkins, C. R. (2011). Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGlu4. ACS Combinatorial Science, 13(2), 159-165. https://doi.org/10.1021/co1000508