Design, synthesis and biological activity of YM-60828 derivatives. Part 2: Potent and orally-bioavailable factor Xa inhibitors based on benzothiadiazine-4-one template

F Hirayama, H Koshio, N Katayama, T Ishihara… - Bioorganic & medicinal …, 2003 - Elsevier
Compound YM-60828 was previously characterized in our laboratory as a potent, selective
and orally-bioavailable Factor Xa (FXa) inhibitor. The L-shape conformation of this …

Design, synthesis and biological activity of YM-60828 derivatives: potent and orally-bioavailable factor Xa inhibitors based on naphthoanilide and …

F Hirayama, H Koshio, T Ishihara, S Watanuki… - Bioorganic & medicinal …, 2002 - Elsevier
Factor Xa (FXa) is a serine protease which plays a pivotal role in the coagulation cascade.
The inhibition of FXa has received great interest as a potential target for the development of …

[HTML][HTML] Novel anthranilamide-based FXa Inhibitors: Drug design, synthesis and biological evaluation

W Wang, J Yuan, X Fu, F Meng, S Zhang, W Xu, Y Xu… - Molecules, 2016 - mdpi.com
Factor Xa (FXa) plays a significant role in the blood coagulation cascade and it has become
a promising target for anticoagulation drugs. Three oral direct FXa inhibitors have been …

Identification of anthranilamide derivatives as potential factor Xa inhibitors: Drug design, synthesis and biological evaluation

J Xing, L Yang, H Li, Q Li, L Zhao, X Wang… - European Journal of …, 2015 - Elsevier
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 …

Synthesis of 3, 4-diaminobenzoyl derivatives as factor Xa inhibitors

J Yang, G Su, Y Ren, Y Chen - European Journal of Medicinal Chemistry, 2015 - Elsevier
Abstract The coagulation factor Xa (FXa) plays a central role in the blood coagulation
cascade. Recent studies have shown that FXa is a particularly attractive target for the …

The discovery of YM-60828: a potent, selective and orally-bioavailable factor Xa inhibitor

F Hirayama, H Koshio, N Katayama, H Kurihara… - Bioorganic & medicinal …, 2002 - Elsevier
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 …

Synthesis and biological activity of novel 1, 2-disubstituted benzene derivatives as factor Xa inhibitors

H Koshio, F Hirayama, T Ishihara, R Shiraki… - Bioorganic & medicinal …, 2005 - Elsevier
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 …

Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold

RA Al-Horani, AY Mehta, UR Desai - European journal of medicinal …, 2012 - Elsevier
Direct inhibition of coagulation factor Xa (FXa) carries significant promise for developing
effective and safe anticoagulants. Although a large number of FXa inhibitors have been …

Design, synthesis and biological evaluation of Piperazinylanthranilamides as potential factor Xa inhibitors

AN Khadse, HH Savsani, RV Chikhale… - Journal of Molecular …, 2022 - Elsevier
Direct inhibition of FXa has emerged as an effective strategy to achieve anticoagulation
maintaining normal hemostasis with minimal bleeding risks. A novel series of …

Design, synthesis, and biological activity of non-basic compounds as factor Xa inhibitors: SAR study of S1 and aryl binding sites

S Komoriya, N Haginoya, S Kobayashi… - Bioorganic & medicinal …, 2005 - Elsevier
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 …