EMAIL THIS PAGE TO A FRIEND

Journal of medicinal chemistry

Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.


PMID 24405333

Abstract

Antithrombotic agents that are inhibitors of factor XIa (FXIa) have the potential to demonstrate robust efficacy with a low bleeding risk profile. Herein, we describe a series of tetrahydroquinoline (THQ) derivatives as FXIa inhibitors. Compound 1 was identified as a potent and selective tool compound for proof of concept studies. It exhibited excellent antithrombotic efficacy in rabbit thrombosis models and did not prolong bleeding times. This demonstrates proof of concept for the FXIa mechanism in animal models with a reversible, small molecule inhibitor.

Related Materials

Product #

Image

Description

Molecular Formula

Add to Cart

F9302
Factor X Activated (Xa) from bovine plasma, aqueous glycerol solution