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 Citations (Scopus)

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

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Tryptases

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., ... 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

Novel pyrazinone inhibitors of mast cell tryptase : Synthesis and SAR evaluation. / Hopkins, Corey; Neuenschwander, Kent; Scotese, Anthony; Jackson, Sharon; Nieduzak, Thaddeus; Pauls, Henry; Liang, Guyan; Sides, Keith; Cramer, Dona; Cairns, Jennifer; Maignan, Sebastien; Mathieu, Magali.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 14, No. 19, 04.10.2004, p. 4819-4823.

Research output: Contribution to journalArticle

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, vol. 14, no. 19, pp. 4819-4823. https://doi.org/10.1016/j.bmcl.2004.07.051
Hopkins, Corey ; Neuenschwander, Kent ; Scotese, Anthony ; Jackson, Sharon ; Nieduzak, Thaddeus ; Pauls, Henry ; Liang, Guyan ; Sides, Keith ; Cramer, Dona ; Cairns, Jennifer ; Maignan, Sebastien ; Mathieu, Magali. / Novel pyrazinone inhibitors of mast cell tryptase : Synthesis and SAR evaluation. In: Bioorganic and Medicinal Chemistry Letters. 2004 ; Vol. 14, No. 19. pp. 4819-4823.
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