title: Novel pyrazinone inhibitors of mast cell tryptase: synthesis and SAR evaluation.
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.
authors.affiliation: Department of Medicinal Chemistry, Drug Innovation and Approval, Aventis Pharmaceuticals, Route 202-206, Bridgewater, NJ 08807, USA. corey.hopkins@aventis.com
authors.forename: Corey
authors.initials: C
authors.lastname: Hopkins
authors.forename: Kent
authors.initials: K
authors.lastname: Neuenschwander
authors.forename: Anthony
authors.initials: A
authors.lastname: Scotese
authors.forename: Sharon
authors.initials: S
authors.lastname: Jackson
authors.forename: Thaddeus
authors.initials: T
authors.lastname: Nieduzak
authors.forename: Henry
authors.initials: H
authors.lastname: Pauls
authors.forename: Guyan
authors.initials: G
authors.lastname: Liang
authors.forename: Keith
authors.initials: K
authors.lastname: Sides
authors.forename: Dona
authors.initials: D
authors.lastname: Cramer
authors.forename: Jennifer
authors.initials: J
authors.lastname: Cairns
authors.forename: Sebastien
authors.initials: S
authors.lastname: Maignan
authors.forename: Magali
authors.initials: M
authors.lastname: Mathieu
mesh_terms: D011719:Pyrazines / Q000138:chemical synthesis* / Q000494:pharmacology; D012697:Serine Endopeptidases / Q000737:chemistry / Q000187:drug effects*; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D053802:Tryptases
chemical_list: D011719:Pyrazines; D015842:Serine Proteinase Inhibitors; D012697:Serine Endopeptidases; D053802:Tryptases