Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors

Q Han, C Dominguez, PFW Stouten… - Journal of medicinal …, 2000 - ACS Publications
Thrombotic diseases are a major cause of death and morbidity. Factor Xa (fXa) plays a vital
role in the regulation of normal homeostasis and abnormal intravascular thrombus …

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 …

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 …

The design and synthesis of noncovalent factor Xa inhibitors

ML Quan, RR Wexler - Current Topics in Medicinal Chemistry, 2001 - ingentaconnect.com
Thrombosis is a major cause of mortality in the industrialized world. Therefore, the control of
blood coagulation has become a major target for new therapeutic agents. One attractive …

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 …

Rational design, synthesis, and structure− activity relationships of novel factor Xa inhibitors:(2-substituted-4-amidinophenyl) pyruvic and-propionic acids

K Sagi, T Nakagawa, M Yamanashi… - Journal of medicinal …, 2003 - ACS Publications
An inhibitor of factor Xa (fXa), the m-substituted benzamidine AXC1578 (1a), was structurally
modified with the aim of increasing its potency. In particular, pyruvic acid and propionic acid …

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 …

Optimization of the β-Aminoester class of factor Xa inhibitors. part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant …

KR Guertin, CJ Gardner, SI Klein, AL Zulli… - Bioorganic & medicinal …, 2002 - Elsevier
Further optimization of the β-aminoester class of factor Xa (fXa) inhibitors is described
culminating in the identification of 9c (FXV673), a potent and selective factor Xa inhibitor with …

Design, synthesis and biological activity of amidinobicyclic compounds (derivatives of DX-9065a) as factor Xa inhibitors: SAR study of S1 and aryl binding sites

S Komoriya, N Kanaya, T Nagahara… - Bioorganic & medicinal …, 2004 - Elsevier
Since factor Xa (fXa) plays a pivotal role in the blood coagulation cascade, inhibition of fXa
is thought to be an effective treatment for a variety of thrombotic events.(2S)-2-[4-[[(3S)-1 …

Structure-based design of potent, amidine-derived inhibitors of factor Xa: evaluation of selectivity, anticoagulant activity, and antithrombotic activity

MR Wiley, LC Weir, S Briggs, NA Bryan… - Journal of medicinal …, 2000 - ACS Publications
To enhance the potency of 1, 2-dibenzamidobenzene-derived inhibitors of factor Xa (fXa),
an amidine substituent was incorporated on one of the benzoyl side chains to interact with …