Synthesis of pyrrolo [3, 2-d] pyrimidineone derivatives as novel FXa inhibitors

J Yang, B Su, R Liao, J Wang, S Bo - Bioorganic & Medicinal Chemistry …, 2023 - Elsevier
Abstract A series of pyrrolo [3, 2-d] pyrimidineone compounds have been designed and
synthesized as novel FXa inhibitors. Bioassay of the tested compounds showed moderate to …

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 …

Synthesis and biological evaluation of Isosteviol derivatives as FXa inhibitors

Y Shi, BW Pan, WC Li, Q Wang, Q Wu, M Pan… - Bioorganic & Medicinal …, 2020 - Elsevier
Firstly, a series of Isosteviol derivatives were synthesized and evaluated for FXa inhibitory
activity. Among these compounds, the inhibitory activity of compounds 22, 35 and 38 on FXa …

Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors

NS Watson, D Brown, M Campbell, C Chan… - Bioorganic & medicinal …, 2006 - Elsevier
A series of novel, non-basic 3-(6-chloronaphth-2-ylsulfonyl) aminopyrrolidin-2-one-based
factor Xa (fXa) inhibitors, incorporating an alanylamide P4 group, was designed and …

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 …

Indoline derivatives II: synthesis and factor Xa (FXa) inhibitory activities

T Noguchi, N Tanaka, T Nishimata, R Goto… - Chemical and …, 2007 - jstage.jst.go.jp
Factor Xa (FXa) is well known to play a pivotal role in blood coagulation, so FXa inhibitor is a
promising drug candidate for prophylaxis and treatment of thromboembolic diseases. In the …

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 …

Design, synthesis and biological evaluation of Piperazinylanthranilamides as potential factor Xa inhibitors

AN Khadse, HH Savsani, RV Chikhale… - Journal of Molecular …, 2022 - Elsevier
Direct inhibition of FXa has emerged as an effective strategy to achieve anticoagulation
maintaining normal hemostasis with minimal bleeding risks. A novel series of …

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 …

1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors

ZJ Jia, Y Wu, W Huang, P Zhang, Y Song… - Bioorganic & medicinal …, 2004 - Elsevier
Using N, N-dialkylated benzamidines as the novel P4 motifs, we have designed and
synthesized a class of 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides as highly potent and …