Novel pyrazinone inhibitors of mast cell tryptase: Synthesis and SAR evaluation

Corey Hopkins, Kent Neuenschwander, Anthony Scotese, Sharon Jackson, Thaddeus Nieduzak, Henry Pauls, Guyan Liang, Keith Sides, Dona Cramer, Jennifer Cairns, Sebastien Maignan, Magali Mathieu

Research output: Contribution to journalArticle

28 Scopus citations

Abstract

In this manuscript, the synthesis and SAR evaluation of a novel pyrazinone class of tryptase inhibitors is described. Chemical optimization of the P1 and P4 groups led to the identification of 7p (K i = 93 nM) as a potent inhibitor of mast cell tryptase.

Original languageEnglish (US)
Pages (from-to)4819-4823
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number19
DOIs
StatePublished - Oct 4 2004

    Fingerprint

Keywords

  • Mast cell tryptase
  • Pyrazinone
  • SAR

ASJC Scopus subject areas

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

Cite this

Hopkins, C., Neuenschwander, K., Scotese, A., Jackson, S., Nieduzak, T., Pauls, H., Liang, G., Sides, K., Cramer, D., Cairns, J., Maignan, S., & Mathieu, M. (2004). Novel pyrazinone inhibitors of mast cell tryptase: Synthesis and SAR evaluation. Bioorganic and Medicinal Chemistry Letters, 14(19), 4819-4823. https://doi.org/10.1016/j.bmcl.2004.07.051