title: Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents.
abstract: A series of novel, highly potent 2-carboxyindole-based factor Xa inhibitors is described. Structural requirements for neutral ligands, which bind in the S1 pocket of factor Xa were investigated with the 2-carboxyindole scaffold. This privileged fragment assembly approach yielded a set of equipotent, selective inhibitors with structurally diverse neutral P1 substituents.
authors.affiliation: Aventis Pharma Deutschland GmbH, D-65926 Frankfurt am Main, Germany. marc.nazare@aventis.com
authors.forename: Marc
authors.initials: M
authors.lastname: Nazaré
authors.forename: Melanie
authors.initials: M
authors.lastname: Essrich
authors.forename: David W
authors.initials: DW
authors.lastname: Will
authors.forename: Hans
authors.initials: H
authors.lastname: Matter
authors.forename: Kurt
authors.initials: K
authors.lastname: Ritter
authors.forename: Matthias
authors.initials: M
authors.lastname: Urmann
authors.forename: Armin
authors.initials: A
authors.lastname: Bauer
authors.forename: Herman
authors.initials: H
authors.lastname: Schreuder
authors.forename: Angela
authors.initials: A
authors.lastname: Dudda
authors.forename: Jörg
authors.initials: J
authors.lastname: Czech
authors.forename: Martin
authors.initials: M
authors.lastname: Lorenz
authors.forename: Volker
authors.initials: V
authors.lastname: Laux
authors.forename: Volkmar
authors.initials: V
authors.lastname: Wehner
mesh_terms: D065427:Factor Xa Inhibitors; D006801:Humans; D007211:Indoles / Q000737:chemistry*; D008968:Molecular Conformation; D015842:Serine Proteinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D065427:Factor Xa Inhibitors; D007211:Indoles; D015842:Serine Proteinase Inhibitors