[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 …

Design and synthesis of glycolic and mandelic acid derivatives as factor Xa inhibitors

T Su, Y Wu, B Doughan, K Kane-Maguire… - Bioorganic & medicinal …, 2001 - Elsevier
A series of glycolic and mandelic acid derivatives was synthesized and investigated for their
factor Xa inhibitory activity. These analogues are highly potent and selective inhibitors …

Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors

MR Becker, WR Ewing, RS Davis, HW Pauls… - Bioorganic & medicinal …, 1999 - Elsevier
Thienopyridine sulfonamide pyrrolidinones were found to be potent and selective inhibitors
of the coagulation cascade enzyme factor Xa. SAR studies led to several compounds that …

[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 …

Discovery of novel tetrahydroisoquinoline derivatives as potent and selective factor Xa inhibitors

H Ueno, K Yokota, J Hoshi, K Yasue, M Hayashi… - Bioorganic & medicinal …, 2005 - Elsevier
A series of novel 2, 7-disubstituted tetrahydroisoquinoline derivatives were designed and
synthesized. Among these derivatives, compounds 1 and 2 (JTV-803) exhibited potent …

Design, synthesis and SAR of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors

K Yoshikawa, T Yoshino, Y Yokomizo, K Uoto… - Bioorganic & medicinal …, 2011 - Elsevier
We previously reported on a series of cyclohexanediamine derivatives as highly potent
factor Xa inhibitors. Herein, we describe the modification of the spacer moiety to discover an …

Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as factor Xa inhibitor

H Nishida, Y MiYAZAKI, Y Kitamura… - Chemical and …, 2001 - jstage.jst.go.jp
Intravascular clot formation is an important factor in a number of cardiovascular diseases.
Therefore, the prevention of blood coagulation has become a major target for new …

Design, synthesis, and biological activity of novel tetrahydropyrazolopyridone derivatives as FXa inhibitors with potent anticoagulant activity

X Sun, Z Hong, M Liu, S Guo, D Yang, Y Wang… - Bioorganic & Medicinal …, 2017 - Elsevier
A series of novel tetrahydropyrazolopyridone derivatives containing 1, 3, 4-triazole,
triazolylmethyl, and partially saturated heterocyclic moieties as P2 binding element was …

[HTML][HTML] Novel isosteviol-based FXa inhibitors: Molecular modeling, in silico design and docking simulation

M Gackowski, B Madriwala, R Studzińska, M Koba - Molecules, 2023 - mdpi.com
Direct oral anticoagulants are an important and relatively new class of synthetic
anticoagulant drugs commonly used for the pharmacotherapy of thromboembolic disorders …

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 …