title: Design of novel, potent, and selective human beta-tryptase inhibitors based on alpha-keto-[1,2,4]-oxadiazoles.
abstract: A series of novel alpha-keto-[1,2,4]-oxadiazoles has been synthesized as human tryptase inhibitors for evaluation as a new class of anti-asthmatic agent. The inhibitor design is focused on using a prime-side hydrophobic pocket and the S2 pocket of beta-tryptase to achieve inhibition potency and selectivity over other serine proteases.
authors.affiliation: Department of Chemistry, Celera, 180 Kimball Way, South San Francisco, CA 94080, USA. csleesammy@gmail.com
authors.forename: Chang-Sun
authors.initials: CS
authors.lastname: Lee
authors.forename: Weili
authors.initials: W
authors.lastname: Liu
authors.forename: Paul A
authors.initials: PA
authors.lastname: Sprengeler
authors.forename: John R
authors.initials: JR
authors.lastname: Somoza
authors.forename: James W
authors.initials: JW
authors.lastname: Janc
authors.forename: David
authors.initials: D
authors.lastname: Sperandio
authors.forename: Jeffrey R
authors.initials: JR
authors.lastname: Spencer
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Green
authors.forename: Mary E
authors.initials: ME
authors.lastname: McGrath
mesh_terms: D018360:Crystallography, X-Ray; D006801:Humans; D007700:Kinetics; D010080:Oxazoles / Q000737:chemistry / Q000494:pharmacology*; D012697:Serine Endopeptidases / Q000187:drug effects*; D053802:Tryptases
chemical_list: D010080:Oxazoles; D012697:Serine Endopeptidases; D053802:Tryptases