Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase

Corey R Hopkins, Mark Czekaj, Steven S. Kaye, Zhongli Gao, James Pribish, Henry Pauls, Guyan Liang, Keith Sides, Dona Cramer, Jennifer Cairns, Yongyi Luo, Heng Keang Lim, Roy Vaz, Sam Rebello, Sebastian Maignan, Alain Dupuy, Magali Mathieu, Julian Levell

Research output: Contribution to journalArticle

29 Citations (Scopus)

Abstract

A new series of novel mast cell tryptase inhibitors is reported, which features the use of an indole structure as the hydrophobic substituent on a m-benzylaminepiperidine template. The best members of this series display good in vitro activity and excellent selectivity against other serine proteases.

Original languageEnglish (US)
Pages (from-to)2734-2737
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume15
Issue number11
DOIs
StatePublished - Jun 2 2005

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Tryptases
Serine Proteases
Bioactivity
Display devices
indole
In Vitro Techniques

ASJC Scopus subject areas

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

Cite this

Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase. / Hopkins, Corey R; Czekaj, Mark; Kaye, Steven S.; Gao, Zhongli; Pribish, James; Pauls, Henry; Liang, Guyan; Sides, Keith; Cramer, Dona; Cairns, Jennifer; Luo, Yongyi; Lim, Heng Keang; Vaz, Roy; Rebello, Sam; Maignan, Sebastian; Dupuy, Alain; Mathieu, Magali; Levell, Julian.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 15, No. 11, 02.06.2005, p. 2734-2737.

Research output: Contribution to journalArticle

Hopkins, CR, Czekaj, M, Kaye, SS, Gao, Z, Pribish, J, Pauls, H, Liang, G, Sides, K, Cramer, D, Cairns, J, Luo, Y, Lim, HK, Vaz, R, Rebello, S, Maignan, S, Dupuy, A, Mathieu, M & Levell, J 2005, 'Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase', Bioorganic and Medicinal Chemistry Letters, vol. 15, no. 11, pp. 2734-2737. https://doi.org/10.1016/j.bmcl.2005.04.002
Hopkins, Corey R ; Czekaj, Mark ; Kaye, Steven S. ; Gao, Zhongli ; Pribish, James ; Pauls, Henry ; Liang, Guyan ; Sides, Keith ; Cramer, Dona ; Cairns, Jennifer ; Luo, Yongyi ; Lim, Heng Keang ; Vaz, Roy ; Rebello, Sam ; Maignan, Sebastian ; Dupuy, Alain ; Mathieu, Magali ; Levell, Julian. / Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase. In: Bioorganic and Medicinal Chemistry Letters. 2005 ; Vol. 15, No. 11. pp. 2734-2737.
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