Add time:08/22/2019         Source:sciencedirect.com

Since Factor Xa (FXa) is well known to play a central role in thrombosis and hemostasis, inhibition of FXa is an attractive target for antithrombotic strategies. As a part of our investigation of a non-peptide, orally available FXa inhibitor, we found that a series of N-[(7-amidino-2-naphthyl)methyl]aniline derivatives possessed potent and selective inhibitory activities. Structure–activity relationship (SAR) of the substituent (R1) on the central aniline moiety suggested that increasing lipophilicity caused a detrimental effect on anticoagulant activity (prothrombin time assay) in plasma. Several compounds bearing a hydrophilic substituent in R1 showed not only potent FXa inhibitory activities but also high anticoagulant activities. The best compound in this series was sulfamoylacetic acid derivative Figure 3, Scheme 1 (YM-60828) which was a potent, selective and orally bioavailable FXa inhibitor and was chosen for clinical development.

We also recommend Trading Suppliers and Manufacturers of YM 435 (cas 138086-00-7). Pls Click Website Link as below: cas 138086-00-7 suppliers