title: Investigation of the terminal P4 domain in a series of D-phenylglycinamide-based factor Xa inhibitors.
abstract: Several P4 domain derivatives of the general d-phenylglycinamide-based scaffold (2) were synthesized and evaluated for their ability to bind to the serine protease factor Xa. Some of the more potent compounds were evaluated for their anticoagulant effects in vitro. A select subset containing various P1 indole constructs was further evaluated for their pharmacokinetic properties after oral administration to rats.
authors.affiliation: Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
authors.forename: Jeffry B
authors.initials: JB
authors.lastname: Franciskovich
authors.forename: John J
authors.initials: JJ
authors.lastname: Masters
authors.forename: Wayne W
authors.initials: WW
authors.lastname: Weber
authors.forename: Valentine J
authors.initials: VJ
authors.lastname: Klimkowski
authors.forename: Michael
authors.initials: M
authors.lastname: Chouinard
authors.forename: Philip R
authors.initials: PR
authors.lastname: Sipes
authors.forename: Lea M
authors.initials: LM
authors.lastname: Johnson
authors.forename: David W
authors.initials: DW
authors.lastname: Snyder
authors.forename: Marcia K
authors.initials: MK
authors.lastname: Chastain
authors.forename: Trelia J
authors.initials: TJ
authors.lastname: Craft
authors.forename: Richard D
authors.initials: RD
authors.lastname: Towner
authors.forename: Donetta S
authors.initials: DS
authors.lastname: Gifford-Moore
authors.forename: Larry L
authors.initials: LL
authors.lastname: Froelich
authors.forename: Jeffrey K
authors.initials: JK
authors.lastname: Smallwood
authors.forename: Ronald S
authors.initials: RS
authors.lastname: Foster
authors.forename: Gerald F
authors.initials: GF
authors.lastname: Smith
authors.forename: John W
authors.initials: JW
authors.lastname: Liebeschuetz
authors.forename: Christopher W
authors.initials: CW
authors.lastname: Murray
authors.forename: Stephen C
authors.initials: SC
authors.lastname: Young
mesh_terms: D000925:Anticoagulants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000990:Antithrombin III / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D015951:Factor Xa / Q000737:chemistry / Q000378:metabolism; D005998:Glycine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D011485:Protein Binding; D013329:Structure-Activity Relationship
chemical_list: D000925:Anticoagulants; C470025:phenylglycinamide; D000990:Antithrombin III; D015951:Factor Xa; D005998:Glycine