title: Investigation of factor Xa inhibitors containing non-amidine S1 elements.
abstract: Several non-amidino S1 derivatives of the 1,2-diaminobenzene-based scaffold (4) were synthesized and evaluated for their ability to bind to the active site and inhibit the human protease factor Xa. A subset of these compounds were also evaluated for their anticoagulant effects in human plasma as measured by prothrombin time (PT).
authors.affiliation: Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. j.franciskovich@lilly.com
authors.forename: Jeffry B
authors.initials: JB
authors.lastname: Franciskovich
authors.forename: John J
authors.initials: JJ
authors.lastname: Masters
authors.forename: Jennifer M
authors.initials: JM
authors.lastname: Tinsley
authors.forename: Trelia J
authors.initials: TJ
authors.lastname: Craft
authors.forename: Larry L
authors.initials: LL
authors.lastname: Froelich
authors.forename: Donetta S
authors.initials: DS
authors.lastname: Gifford-Moore
authors.forename: Valentine J
authors.initials: VJ
authors.lastname: Klimkowski
authors.forename: Jeffrey K
authors.initials: JK
authors.lastname: Smallwood
authors.forename: Gerald F
authors.initials: GF
authors.lastname: Smith
authors.forename: Tommy
authors.initials: T
authors.lastname: Smith
authors.forename: Richard R
authors.initials: RR
authors.lastname: Towner
authors.forename: Leonard C
authors.initials: LC
authors.lastname: Weir
authors.forename: Michael R
authors.initials: MR
authors.lastname: Wiley
mesh_terms: D000925:Anticoagulants / Q000138:chemical synthesis* / Q000494:pharmacology; D001555:Benzene Derivatives / Q000138:chemical synthesis* / Q000494:pharmacology; D001665:Binding Sites; D001777:Blood Coagulation / Q000187:drug effects; D015951:Factor Xa / Q000378:metabolism; D065427:Factor Xa Inhibitors; D006801:Humans; D008958:Models, Molecular; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D011485:Protein Binding; D011517:Prothrombin Time; D013329:Structure-Activity Relationship
chemical_list: D000925:Anticoagulants; D001555:Benzene Derivatives; D065427:Factor Xa Inhibitors; D011480:Protease Inhibitors; D015951:Factor Xa