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 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 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 …

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 …

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 …

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 (1H)-one derivatives …

Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity

P Zhang, L Bao, JF Zuckett, ZJ Jia, J Woolfrey… - Bioorganic & medicinal …, 2004 - Elsevier
Compound 2 containing an aminomethylbenzoyl moiety as the S4 binding motif was
synthesized in order to modulate hydrophlicity of anthranilamide-based factor Xa inhibitors …

Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants

PYS Lam, CG Clark, R Li, DJP Pinto… - Journal of medicinal …, 2003 - ACS Publications
As part of an ongoing effort to prepare orally active factor Xa inhibitors using structure-based
drug design techniques and molecular recognition principles, a systematic study has been …

Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors

B Ye, DO Arnaiz, YL Chou, BD Griedel… - Journal of medicinal …, 2007 - ACS Publications
There remains a high unmet medical need for a safe oral therapy for thrombotic disorders.
The serine protease factor Xa (fXa), with its central role in the coagulation cascade, is …

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 …