Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4)

Rocco D. Gogliotti, Anna L. Blobaum, Ryan M. Morrison, J. Scott Daniels, James M. Salovich, Yiu Yin Cheung, Alice L. Rodriguez, Matthew T. Loch, P. Jeffrey Conn, Craig W. Lindsley, Colleen M. Niswender, Corey R. Hopkins

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Abstract

Herein we report the synthesis and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as novel positive allosteric modulators of mGlu4. We detail our work towards finding phenyl replacements for the core scaffold of previously reported phenyl sulfonamides and phenyl sulfone compounds. Our efforts culminated in the identification of N-(1-((3,4-dimethylphenyl)sulfonyl)-1H-pyrrol-3-yl)picolinamide as a potent PAM of mGlu4.

Original languageEnglish (US)
Pages (from-to)2984-2987
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume26
Issue number13
DOIs
StatePublished - Jul 1 2016

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Keywords

  • Metabotropic glutamate receptor 4
  • PK
  • Phenyl replacement
  • Positive allosteric modulator (PAM)
  • Pyrrole sulfonamide

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Gogliotti, R. D., Blobaum, A. L., Morrison, R. M., Daniels, J. S., Salovich, J. M., Cheung, Y. Y., Rodriguez, A. L., Loch, M. T., Conn, P. J., Lindsley, C. W., Niswender, C. M., & Hopkins, C. R. (2016). Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4). Bioorganic and Medicinal Chemistry Letters, 26(13), 2984-2987. https://doi.org/10.1016/j.bmcl.2016.05.029