Design and synthesis of highly constrained factor Xa inhibitors: amidine-Substituted bis (benzoyl)-,-diazepan-2-ones and bis (benzylidene)-bis (gem-dimethyl) …

J Cui, D Crich, D Wink, M Lam, AL Rheingold… - Bioorganic & medicinal …, 2003 - Elsevier
Two conformationally constrained templates have been designed to provide selective
inhibitors of the coagulation cascade serine protease, Factor Xa (FXa). The most active …

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 …

Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors

T Ishihara, N Seki, F Hirayama, M Orita… - Bioorganic & medicinal …, 2007 - Elsevier
We describe here our investigation of a new series of orally active fXa inhibitors based on a
prodrug strategy. Solid-phase parallel synthesis identified a unique series of fXa inhibitors …

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 …

Structure-and property-based design of factor Xa inhibitors: pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs

RJ Young, M Campbell, AD Borthwick, D Brown… - Bioorganic & medicinal …, 2006 - Elsevier
Structure-based drug design was exploited in the synthesis of 3-(6-chloronaphth-2-
ylsulfonyl) aminopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating an …

Structural requirements for factor Xa inhibition by 3-oxybenzamides with neutral P1 substituents: combining X-ray crystallography, 3D-QSAR, and tailored scoring …

H Matter, DW Will, M Nazaré, H Schreuder… - Journal of medicinal …, 2005 - ACS Publications
The design, synthesis, and structure− activity relationship of 3-oxybenzamides as potent
inhibitors of the coagulation protease factor Xa are described on the basis of X-ray …

Synthesis, Characterization, and Structure− Activity Relationships of Amidine-Substituted (Bis) benzylidene-Cycloketone Olefin Isomers as Potent and Selective Factor …

WJ Guilford, KJ Shaw, JL Dallas… - Journal of medicinal …, 1999 - ACS Publications
Factor Xa (FXa) is a trypsin-like serine protease that plays a key role in blood coagulation
linking the intrinsic and extrinsic pathways to the final common pathway of the coagulation …

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 …

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 …

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 …