A novel series of potent and efficacious factor Xa inhibitors which possesses sulfoximine
moiety as novel S4 binding element in anthranilamide chemotype has been identified. Lead …

Compound 2 containing an aminomethylbenzoyl moiety as the S4 binding motif was
synthesized in order to modulate hydrophlicity of anthranilamide-based factor Xa inhibitors …

Anthranilamide-based benzamidine compound 4 and its N-substituted analogs were
designed and examined as factor Xa inhibitors using substituted benzamidines as …

The coagulation enzyme factor Xa (fXa) plays a crucial role in the blood coagulation
cascade. In this study, three-dimensional fragment based drug design (FBDD) combined …

Anthranilamides 4 and 5 were designed and synthesized as selective and orally
bioavailable factor Xa inhibitors. Structural modifications aimed at lowering their lipophilicity …

Compound 7 was identified as the active metabolite of 6 by HPLC and mass spectral
analysis. Modification of lead compound 7 by transformation of its N-oxide 6–6 biaryl ring …

Factor Xa (fXa) is a serine protease that plays a pivotal role in the coagulation cascade. High-
throughput screening of the Yamanouchi compound library yielded lead compound 1 with …

A novel series of potent and efficacious factor Xa inhibitors which possesses
pyrrole/indole/thiazole moieties as S4 binding element was identified. Compound 7b …

To develop a novel and effective anticoagulant with potent and selective factor Xa (FXa)
inhibitory activity, a new series of cinnamyl derivatives with enhanced lipophilicity and …

Our exploratory study was based on the concept that a non-amidine factor Xa (fXa) inhibitor
is suitable for an orally available anticoagulant. We synthesized and evaluated a series of N …