title: Anthranilamide inhibitors of factor Xa.
abstract: SAR about the B-ring of a series of N(2)-aroyl anthranilamide factor Xa (fXa) inhibitors is described. B-ring o-aminoalkylether and B-ring p-amine probes of the S1' and S4 sites, respectively, afforded picomolar fXa inhibitors that performed well in in vitro anticoagulation assays.
authors.affiliation: Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. mendel_david@lilly.com
authors.forename: David
authors.initials: D
authors.lastname: Mendel
authors.forename: Angela L
authors.initials: AL
authors.lastname: Marquart
authors.forename: Sajan
authors.initials: S
authors.lastname: Joseph
authors.forename: Philip
authors.initials: P
authors.lastname: Waid
authors.forename: Ying K
authors.initials: YK
authors.lastname: Yee
authors.forename: Anne Louise
authors.initials: AL
authors.lastname: Tebbe
authors.forename: Andrew M
authors.initials: AM
authors.lastname: Ratz
authors.forename: David K
authors.initials: DK
authors.lastname: Herron
authors.forename: Theodore
authors.initials: T
authors.lastname: Goodson
authors.forename: John J
authors.initials: JJ
authors.lastname: Masters
authors.forename: Jeffry B
authors.initials: JB
authors.lastname: Franciskovich
authors.forename: Jennifer M
authors.initials: JM
authors.lastname: Tinsley
authors.forename: Michael R
authors.initials: MR
authors.lastname: Wiley
authors.forename: Leonard C
authors.initials: LC
authors.lastname: Weir
authors.forename: Jeffrey A
authors.initials: JA
authors.lastname: Kyle
authors.forename: Valentine J
authors.initials: VJ
authors.lastname: Klimkowski
authors.forename: Gerald F
authors.initials: GF
authors.lastname: Smith
authors.forename: Richard D
authors.initials: RD
authors.lastname: Towner
authors.forename: Larry L
authors.initials: LL
authors.lastname: Froelich
authors.forename: John
authors.initials: J
authors.lastname: Buben
authors.forename: Trelia J
authors.initials: TJ
authors.lastname: Craft
mesh_terms: D000925:Anticoagulants / Q000737:chemistry; D000990:Antithrombin III / Q000138:chemical synthesis* / Q000737:chemistry; D001665:Binding Sites; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D065427:Factor Xa Inhibitors; D005456:Fluorescent Dyes / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D007700:Kinetics; D008956:Models, Chemical; D008968:Molecular Conformation; D013329:Structure-Activity Relationship; D062367:ortho-Aminobenzoates / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D000925:Anticoagulants; D065427:Factor Xa Inhibitors; D005456:Fluorescent Dyes; D062367:ortho-Aminobenzoates; D000990:Antithrombin III; C000219:anthranilamide