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European journal of medicinal chemistry v.143, 2018년, pp.1997 - 2004   SCI SCIE
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Thieno[2,3-b]pyridine derivatives are potent anti-platelet drugs, inhibiting platelet activation, aggregation and showing synergy with aspirin

Binsaleh, Naif K. (School of Healthcare Science, Manchester Metropolitan University, Manchester M1 5GD, UK ) ; Wigley, Catherine A. (School of Healthcare Science, Manchester Metropolitan University, Manchester M1 5GD, UK ) ; Whitehead, Kathryn A. (School of Healthcare Science, Manchester Metropolitan University, Manchester M1 5GD, UK ) ; van Rensburg, Michelle (School of Chemical Sciences, The University of Auckland, New Zealand ) ; Reynisson, Johannes (School of Chemical Sciences, The University of Auckland, New Zealand ) ; Pilkington, Lisa I. (School of Chemical Sciences, The University of Auckland, New Zealand ) ; Barker, David (School of Chemical Sciences, The University of Auckland, New Zealand ) ; Jones, Sarah (School of Healthcare Science, Manchester Metropolitan University, Manchester M1 5GD, UK ) ; Dempsey-Hibbert, Nina C. (School of Healthcare Science, Manchester Metropolitan University, Manchester M1 5GD, UK ) ;
  • 초록  

    Abstract 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. Highlights Thieno[2,3- b ]pyridines inhibited platelet activation and aggregation. Thieno[2,3- b ]pyridines showed synergy with aspirin. Tested compounds had greater activity to clinically used thieno[3,2- c ]pyridines. Thieno[2,3- b ]pyridines have been found to be a novel class of P2Y 12 inhibitors. Graphical abstract [DISPLAY OMISSION]


  • 주제어

    Thienopyridine .   Platelets .   Thrombosis .   Clopidogrel .   Aspirin.  

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