Discovery of novel, potent, isosteviol-based antithrombotic agents.

Clicks: 368
ID: 81113
2019
Article Quality & Performance Metrics
Overall Quality Improving Quality
0.0 /100
Combines engagement data with AI-assessed academic quality
AI Quality Assessment
Not analyzed
Abstract
Thrombosis is a pathological coagulation process and can lead to many serious thrombotic diseases. Here, we report a novel potent antithrombotic compound (6k) based on isosteviol with anticoagulant and antiplatelet activities. 6k selectively inhibited FXa (K = 0.015 μM) against a panel of serine proteases and showed excellent anticoagulant activity (significant prolongation of ex vivo PT and aPTT over the vehicle, p < 0.01). 6k also significantly inhibited ADP-induced platelet aggregation in rats relative to the vehicle (p < 0.01). Furthermore, 6k exhibited potent ex vivo and in vivo antithrombotic activity in rats relative to the vehicle (p < 0.01 and p < 0.0001, respectively). Novel structure 6k, with potent antithrombotic activity, is expected to lead a promising approach for the development of antithrombotic agents.
Reference Key
chen2019discoveryeuropean Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Chen, Peng;Zhang, Dianwen;Li, Meng;Wu, Qiong;Lam, Yuko P Y;Guo, Yan;Chen, Chen;Bai, Nan;Malhotra, Shipra;Li, Wei;O'Connor, Peter B;Fu, Hongzheng;
Journal European journal of medicinal chemistry
Year 2019
DOI
S0223-5234(19)30874-8
URL
Keywords
biopolymers biomass green chemistry organocatalysis renewable resources

Citations

No citations found. To add a citation, contact the admin at info@scimatic.org

Comments

No comments yet. Be the first to comment on this article.