title: Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors.
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.
authors.affiliation: Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA. david.sperandio@gilead.com
authors.forename: David
authors.initials: D
authors.lastname: Sperandio
authors.forename: Vincent W-F
authors.initials: VW
authors.lastname: Tai
authors.forename: Julia
authors.initials: J
authors.lastname: Lohman
authors.forename: Bernie
authors.initials: B
authors.lastname: Hirschbein
authors.forename: Rohan
authors.initials: R
authors.lastname: Mendonca
authors.forename: Chang-Sun
authors.initials: CS
authors.lastname: Lee
authors.forename: Jeffrey R
authors.initials: JR
authors.lastname: Spencer
authors.forename: James
authors.initials: J
authors.lastname: Janc
authors.forename: Margaret
authors.initials: M
authors.lastname: Nguyen
authors.forename: Jerlyn
authors.initials: J
authors.lastname: Beltman
authors.forename: Paul
authors.initials: P
authors.lastname: Sprengeler
authors.forename: Heleen
authors.initials: H
authors.lastname: Scheerens
authors.forename: Tong
authors.initials: T
authors.lastname: Lin
authors.forename: Liang
authors.initials: L
authors.lastname: Liu
authors.forename: Ashwini
authors.initials: A
authors.lastname: Gadre
authors.forename: Alisha
authors.initials: A
authors.lastname: Kellogg
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Green
authors.forename: Mary E
authors.initials: ME
authors.lastname: McGrath
mesh_terms: D000284:Administration, Oral; D001682:Biological Availability; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D012697:Serine Endopeptidases / Q000187:drug effects*; D013329:Structure-Activity Relationship; D053802:Tryptases
chemical_list: D004791:Enzyme Inhibitors; D012697:Serine Endopeptidases; D053802:Tryptases