title: Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
abstract: A series of nonguanidine N1-activated C4-carboxy azetidinone tryptase inhibitors was prepared by solid-phase methodology to quickly assess the SAR associated with distal functionality on the N1-activating group. From these studies, potent inhibitors with improved specificity were discovered.
authors.affiliation: The Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. james.sutton@bms.com
authors.forename: James C
authors.initials: JC
authors.lastname: Sutton
authors.forename: Scott A
authors.initials: SA
authors.lastname: Bolton
authors.forename: Malcolm E
authors.initials: ME
authors.lastname: Davis
authors.forename: Karen S
authors.initials: KS
authors.lastname: Hartl
authors.forename: Bruce
authors.initials: B
authors.lastname: Jacobson
authors.forename: Arvind
authors.initials: A
authors.lastname: Mathur
authors.forename: Martin L
authors.initials: ML
authors.lastname: Ogletree
authors.forename: William A
authors.initials: WA
authors.lastname: Slusarchyk
authors.forename: Robert
authors.initials: R
authors.lastname: Zahler
authors.forename: Steven M
authors.initials: SM
authors.lastname: Seiler
authors.forename: Gregory S
authors.initials: GS
authors.lastname: Bisacchi
mesh_terms: D001384:Azetidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D008958:Models, Molecular; D012697:Serine Endopeptidases / Q000737:chemistry / Q000187:drug effects*; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D053802:Tryptases
chemical_list: C116379:2-azetidinone; D001384:Azetidines; D015842:Serine Proteinase Inhibitors; D012697:Serine Endopeptidases; D053802:Tryptases