Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors

David Sperandio; Vincent W-F Tai; Julia Lohman; Bernie Hirschbein; Rohan Mendonca; Chang-Sun Lee; Jeffrey R Spencer; James Janc; Margaret Nguyen; Jerlyn Beltman; Paul Sprengeler; Heleen Scheerens; Tong Lin; Liang Liu; Ashwini Gadre; Alisha Kellogg; Michael J Green; Mary E McGrath

doi:10.1016/j.bmcl.2006.04.088

Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors

Bioorg Med Chem Lett. 2006 Aug 1;16(15):4085-9. doi: 10.1016/j.bmcl.2006.04.088. Epub 2006 May 24.

Authors

David Sperandio¹, Vincent W-F Tai, Julia Lohman, Bernie Hirschbein, Rohan Mendonca, Chang-Sun Lee, Jeffrey R Spencer, James Janc, Margaret Nguyen, Jerlyn Beltman, Paul Sprengeler, Heleen Scheerens, Tong Lin, Liang Liu, Ashwini Gadre, Alisha Kellogg, Michael J Green, Mary E McGrath

Affiliation

¹ Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA. david.sperandio@gilead.com

PMID: 16725321
DOI: 10.1016/j.bmcl.2006.04.088

Abstract

The synthesis of novel [1,2,4]oxadiazoles and their structure-activity relationship (SAR) for the inhibition of tryptase and related serine proteases is presented. Elaboration of the P'-side afforded potent, selective, and orally bioavailable tryptase inhibitors.

MeSH terms

Administration, Oral
Biological Availability
Enzyme Inhibitors / administration & dosage
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Models, Molecular
Serine Endopeptidases / drug effects*
Structure-Activity Relationship
Tryptases

Substances

Enzyme Inhibitors
Serine Endopeptidases
Tryptases