title: Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase.
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.
authors.affiliation: Department of Medicinal Chemistry, Aventis Pharmaceuticals, Bridgewater, NJ 08807, USA. corey.hopkins@aventis.com
authors.forename: Corey R
authors.initials: CR
authors.lastname: Hopkins
authors.forename: Mark
authors.initials: M
authors.lastname: Czekaj
authors.forename: Steven S
authors.initials: SS
authors.lastname: Kaye
authors.forename: Zhongli
authors.initials: Z
authors.lastname: Gao
authors.forename: James
authors.initials: J
authors.lastname: Pribish
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: Yongyi
authors.initials: Y
authors.lastname: Luo
authors.forename: Heng-Keang
authors.initials: HK
authors.lastname: Lim
authors.forename: Roy
authors.initials: R
authors.lastname: Vaz
authors.forename: Sam
authors.initials: S
authors.lastname: Rebello
authors.forename: Sebastian
authors.initials: S
authors.lastname: Maignan
authors.forename: Alain
authors.initials: A
authors.lastname: Dupuy
authors.forename: Magali
authors.initials: M
authors.lastname: Mathieu
authors.forename: Julian
authors.initials: J
authors.lastname: Levell
mesh_terms: D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008407:Mast Cells / Q000201:enzymology*; 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