title: Isoxazolines and isoxazoles as factor Xa inhibitors.
abstract: 3,4,5-Trisubstituted isoxazolines (2) and isoxazoles (3) were prepared and evaluated for their in vitro and in vivo antithrombotic efficacy. They were compared to 3,5,5-trisubstituted isoxazolines (1) for Factor Xa selectivity and potency. They were also compared in an arterio-venous (A-V) shunt model of thrombosis.
authors.affiliation: The DuPont Pharmaceuticals Company, Wilmington, Delaware 19880-0500, USA. james.r.pruitt@dupontpharma.com
authors.forename: J R
authors.initials: JR
authors.lastname: Pruitt
authors.forename: D J
authors.initials: DJ
authors.lastname: Pinto
authors.forename: M J
authors.initials: MJ
authors.lastname: Estrella
authors.forename: L L
authors.initials: LL
authors.lastname: Bostrom
authors.forename: R M
authors.initials: RM
authors.lastname: Knabb
authors.forename: P C
authors.initials: PC
authors.lastname: Wong
authors.forename: M R
authors.initials: MR
authors.lastname: Wright
authors.forename: R R
authors.initials: RR
authors.lastname: Wexler
mesh_terms: D000818:Animals; D018360:Crystallography, X-Ray; D065427:Factor Xa Inhibitors; D007555:Isoxazoles / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D008958:Models, Molecular; D011817:Rabbits; D015842:Serine Proteinase Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013927:Thrombosis / Q000517:prevention & control
chemical_list: D065427:Factor Xa Inhibitors; D007555:Isoxazoles; D015842:Serine Proteinase Inhibitors