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

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ID: 81113
2019
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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.
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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

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