Contemporary developments in the discovery of selective factor Xa inhibitors: A review

NR Patel, DV Patel, PR Murumkar, MR Yadav - European journal of …, 2016 - Elsevier
Thrombosis is a leading cause of death in cardiovascular diseases such as myocardial
infarction (MI), unstable angina and acute coronary syndrome (ACS) in the industrialized …

Total synthesis of virgatolide B

PA Hume, DP Furkert, MA Brimble - Organic Letters, 2013 - ACS Publications
The first total synthesis of the benzannulated spiroketal virgatolide A is presented. Key
features include sp3–sp2 Suzuki coupling of an enantiomerically enriched β …

Design, synthesis and structure–activity relationship of oxazolidinone derivatives containing novel S4 ligand as FXa inhibitors

Y Zhao, M Jiang, S Zhou, S Wu, X Zhang, L Ma… - European journal of …, 2015 - Elsevier
A novel series of potent and efficacious factor Xa inhibitors which possesses
pyrrole/indole/thiazole moieties as S4 binding element was identified. Compound 7b …

Design, synthesis, and structure–activity relationship of novel and effective apixaban derivatives as FXa inhibitors containing 1, 2, 4-triazole/pyrrole derivatives as P2 …

Y Wang, X Sun, D Yang, Z Guo, X Fan, M Nie… - Bioorganic & Medicinal …, 2016 - Elsevier
Four series of novel and potent FXa inhibitors possessing the 1, 2, 4-triazole moiety and
pyrrole moiety as P2 binding element and dihydroimidazole/tetrahydropyrimidine groups as …

一种新型凝血因子Xa 抑制剂的合成与活性研究

林轲倪, 杨根生 - 广东化工, 2014 - cqvip.com
抗凝血药物是目前预防和治疗心血管疾病的一种主要手段, 而凝血因子Xa 抑制剂被认为是目前
为止最为理想的一种抗凝血药物, 具有口服吸收好, 耐受性佳, 药物代谢动力学和药效学特性可以 …

Synthesis and antibacterial activity evaluation of C-5 side chain modified analogues of FYL-66, a potential agent against methicillin-resistant Staphylococcus aureus

X Yang, Z Li, Z Wang, Z Sang, H Long, J Tang… - …, 2015 - pubs.rsc.org
FYL-66 and its hydrochloride FYL-67 have been identified as new chemical entities (NCE)
with pronounced in vitro and in vivo activities against MRSA and MSSA. Aiming to explore …

Advances in inhibitors of FXa

L Guo, S Ma - Current Drug Targets, 2015 - ingentaconnect.com
Thromboembolic diseases such as deep vein thrombosis (DVT), pulmonary embolism (PE),
myocardial infarction (MI) and ischemic strokes are mainly responsible for people's morbidity …

Orally active zwitterionic factor Xa inhibitors with long duration of action

A Mochizuki, T Nagata, H Kanno, D Takano… - Bioorganic & medicinal …, 2011 - Elsevier
We have optimized 2-aminomethylphenylamine derivative as a factor Xa inhibitor. Several
polar functional groups were introduced in the central phenyl ring, and we focused on zwitter …

Design and synthesis of 3-arylisoxazoline-5-carboxamide and 3-arylisoxazoline-5-acetamide libraries as potential factor Xa inhibitors

JF Quinn, BT Gregg, DB Kitchen… - Letters in Drug …, 2012 - ingentaconnect.com
Two synthetic libraries based on a core isoxazoline motif have been designed and prepared
specifically to probe the S1 and S4 binding pockets of the Factor Xa enzyme active sites. A …

AutoGPA-Based 3D-QSAR Modeling and Molecular Docking Study on Factor Xa Inhibitors as Anticoagulant Agents

FY Guo, QY Yan, K Lin, WY Hong… - MATEC Web of …, 2016 - matec-conferences.org
The three-dimensional-quantitative structure activity relationship (3D-QSAR) studies were
performed on a series of direct factor Xa (FXa) inhibitors using AutoGPA-based modeling …