Synthesis and Thrombin, Factor Xa and U46619 Inhibitory Effects of Non-Amidino and Amidino N²-Thiophenecarbonyl- and N²-Tosylanthranilamides.

Clicks: 254
ID: 3464
2017
Article Quality & Performance Metrics
Overall Quality
Not rated
Combines reader engagement with the AI quality analysis. This article has not been analysed, so there is no overall score — reader engagement is measured and shown alongside.
AI Quality Assessment
Not analyzed
Readership in this journal
Popular

Ranked #244 of 430 articles by views in International journal of molecular sciences

Most read Least read

Bar heights use a square-root scale. Only the 120 most-read articles are drawn; the journal has 430 in total.

Mint this article as an NFT
Not yet minted

Create a permanent, verifiable on-chain record of this article on the Scimatic Network. The NFT is held in your Journament account, and you can withdraw it to your own wallet at any time.

5 SUSD one-off · no wallet required
Sign in to mint
Abstract
Thrombin (factor IIa) and factor Xa (FXa) are key enzymes at the junction of the intrinsic and extrinsic coagulation pathways and are the most attractive pharmacological targets for the development of novel anticoagulants. Twenty non-amidino ²-thiophencarbonyl- and ²-tosyl anthranilamides - and six amidino ²-thiophencarbonyl- and ²-tosylanthranilamides - were synthesized to evaluate their activated partial thromboplastin time (aPTT) and prothrombin time (PT) using human plasma at a concentration of 30 µg/mL in vitro. As a result, compounds , , and - were selected to study the further antithrombotic activity. The anticoagulant properties of , , and - significantly exhibited a concentration-dependent prolongation of in vitro PT and aPTT, in vivo bleeding time, and ex vivo clotting time. These compounds concentration-dependently inhibited the activities of thrombin and FXa and inhibited the generation of thrombin and FXa in human endothelial cells. In addition, data showed that , , and - significantly inhibited thrombin catalyzed fibrin polymerization and mouse platelet aggregation and inhibited platelet aggregation induced by U46619 in vitro and ex vivo. Among the derivatives evaluated, -(3'-amidinophenyl)-2-((thiophen-2''-yl)carbonylamino)benzamide () was the most active compound.
Reference Key
lee2017synthesisinternational Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Lee, Soo Hyun;Lee, Wonhwa;Nguyen, ThiHa;Um, Il Soo;Bae, Jong-Sup;Ma, Eunsook;
Journal International journal of molecular sciences
Year 2017
DOI
E1144
URL
Keywords Keywords not found

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.