Design, synthesis and biological evaluation of novel 2, 3-dihydroquinazolin-4 (1H)-one derivatives as potential fXa inhibitors

J Xing, L Yang, Y Yang, L Zhao, Q Wei, J Zhang… - European Journal of …, 2017 - Elsevier
Coagulation factor Xa (fXa) is a particularly attractive target for the development of effective
and safe anticoagulants. In this study, novel 2, 3-dihydroquinazolin-4 (1 H)-one derivatives …

Design, synthesis and biological evaluation of anthranilamide derivatives as potential factor Xa (fXa) inhibitors

J Xing, L Yang, J Zhou, H Zhang - Bioorganic & Medicinal Chemistry, 2018 - Elsevier
Factor Xa (fXa) is a crucial player in various thromboembolic disorders. Inhibition of fXa can
provide safe and effective antithrombotic effects. In this study, a series of anthranilamide …

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 …

[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 …

[HTML][HTML] Identification of new pyrazolyl piperidine molecules as factor Xa inhibitors: Design, synthesis, in silico, and biological evaluation

RH Rayani, JY Soni, DR Parmar, RV Kusurkar… - Results in …, 2022 - Elsevier
Abstract Coagulation factor Xa (FXa), a serine endopeptidase is a common coagulation
factor activated as a result of the initiation of both intrinsic and extrinsic blood coagulation …

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 …

Discovery of R-142086 as a factor Xa (fXa) inhibitor: Syntheses and structure–activity relationships of cinnamyl derivatives

T Noguchi, N Tanaka, T Nishimata, R Goto… - Chemical and …, 2009 - jstage.jst.go.jp
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 …

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 …

Indoline derivatives II: synthesis and factor Xa (FXa) inhibitory activities

T Noguchi, N Tanaka, T Nishimata, R Goto… - Chemical and …, 2007 - jstage.jst.go.jp
Factor Xa (FXa) is well known to play a pivotal role in blood coagulation, so FXa inhibitor is a
promising drug candidate for prophylaxis and treatment of thromboembolic diseases. In the …

Discovery of a Tetrahydropyrimidin-2(1H)-one Derivative (TAK-442) as a Potent, Selective, and Orally Active Factor Xa Inhibitor

T Fujimoto, Y Imaeda, N Konishi, K Hiroe… - Journal of medicinal …, 2010 - ACS Publications
Coagulation enzyme factor Xa (FXa) is a particularly promising target for the development of
new anticoagulant agents. We previously reported the imidazo [1, 5-c] imidazol-3-one …