Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as a factor Xa inhibitor II. Substituent effect on biological activities

H Nishida, Y Miyazaki, T Mukaihira, F Saitoh… - Chemical and …, 2002 - jstage.jst.go.jp
Intravascular clot formation is an important event in a number of cardiovascular diseases.
The prevention of blood coagulation has become a major target for new therapeutic agents …

The development of new low-molecular-weight factor Xa inhibitors that are potential anticoagulants

DG Tovbin, DN Tarasov, DV Malakhov… - Current Drug …, 2022 - ingentaconnect.com
Background: Despite the introduction of direct oral anticoagulants, the search for new oral
anticoagulants remains an urgent task. Objective: By using docking and scoring, based on …

Tetrahydro-isoquinoline-based factor Xa inhibitors

R Kucznierz, F Grams, H Leinert… - Journal of medicinal …, 1998 - ACS Publications
Derivatives of (2-amidino-1, 2, 3, 4-tetrahydro-isoquinolin-7-yloxy) phenylacetic acid (TIPAC)
were developed as inhibitors of factor Xa (fXa). The compounds are prepared using 15 …

Discovery of N-[(1R, 2S, 5S)-2-{[(5-chloroindol-2-yl) carbonyl] amino}-5-(dimethylcarbamoyl) cyclohexyl]-5-methyl-4, 5, 6, 7-tetrahydrothiazolo [5, 4-c] pyridine-2 …

T Nagata, T Yoshino, N Haginoya, K Yoshikawa… - Bioorganic & medicinal …, 2009 - Elsevier
In the early 1990's, we reported on the low-molecular selective fXa inhibitor DX-9065a
having two amidino groups. However, it had poor oral bioavailability due to its strong basic …

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 …

Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors

P Zhang, JF Zuckett, J Woolfrey, K Tran… - Bioorganic & medicinal …, 2002 - Elsevier
Monoamidine FXa inhibitors 3 were designed and synthesized. SAR studies and molecular
modeling led to the design of conformationally constrained diaryl ethers 4 and 5, as well as …

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 …

Pharmacological characterization of the active synthetic factor Xa inhibitors M55551 and M55165

Y Hosaka, M Matsumoto, M Shinozaki, T Ohno… - European journal of …, 2006 - Elsevier
Factor Xa plays an important role in blood coagulation and is widely regarded as an
attractive target for antithrombotic drug development. M55551 and M55165 (1-arylsulfonyl-3 …

FXa direct synthetic inhibitors

FC Zacconi - Anticoagulant Drugs, 2018 - books.google.com
Abstract Factor Xa (FXa) is an enzyme belonging to the serine protease family which plays a
vital role in hemostasis, being an essential part in the blood-clotting cascade by catalyzing …

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 …