4.7 Article

Thieno[2,3-b]pyridine derivatives are potent anti-platelet drugs, inhibiting platelet activation, aggregation and showing synergy with aspirin

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 143, Issue -, Pages 1997-2004

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2017.11.014

Keywords

Thienopyridine; Platelets; Thrombosis; Clopidogrel; Aspirin

Funding

  1. Saudi Arabian Cultural Bureau on behalf of University of Hail
  2. Manchester Metropolitan University Healthcare Science Research Centre
  3. Auckland Medical Research Foundation

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Drugs which inhibit platelet function are commonly used to prevent blood clot formation in patients with Acute Coronary Syndromes (ACS) or those at risk of stroke. The thieno[3,2-c]pyridine class of therapeutic agents, of which clopidogrel is the most commonly used, target the P2Y(12) receptor, and are often used in combination with acetylsalicylic acid (ASA). Six thieno[2,3-b]pyridine were assessed for in vitro anti-platelet activity; all derivatives showed effects on both platelet activation and aggregation, and showed synergy with ASA. Some compounds demonstrated greater activity when compared to clopidogrel. These compounds, therefore, represent potential novel P2Y(12) inhibitors for improved treatment for patients. (C) 2017 Elsevier Masson SAS. All rights reserved.

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