Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents.
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.
Nazaré
Marc
M
Aventis Pharma Deutschland GmbH, D-65926 Frankfurt am Main, Germany. marc.nazare@aventis.com
Essrich
Melanie
M
Will
David W
DW
Matter
Hans
H
Ritter
Kurt
K
Urmann
Matthias
M
Bauer
Armin
A
Schreuder
Herman
H
Dudda
Angela
A
Czech
Jörg
J
Lorenz
Martin
M
Laux
Volker
V
Wehner
Volkmar
V
D065427:Factor Xa Inhibitors; D006801:Humans; D007211:Indoles / Q000737:chemistry*; D008968:Molecular Conformation; D015842:Serine Proteinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*
D065427:Factor Xa Inhibitors; D007211:Indoles; D015842:Serine Proteinase Inhibitors