Binsaleh Naif K, Wigley Catherine A, Whitehead Kathryn A, van Rensburg Michelle, Reynisson Johannes, Pilkington Lisa I, Barker David, Jones Sarah, Dempsey-Hibbert Nina C
School of Healthcare Science, Manchester Metropolitan University, Manchester M1 5GD, UK.
School of Chemical Sciences, The University of Auckland, New Zealand.
Eur J Med Chem. 2018 Jan 1;143:1997-2004. doi: 10.1016/j.ejmech.2017.11.014. Epub 2017 Nov 7.
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 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 inhibitors for improved treatment for patients.
抑制血小板功能的药物通常用于预防急性冠状动脉综合征(ACS)患者或有中风风险的患者形成血栓。噻吩并[3,2-c]吡啶类治疗药物(其中氯吡格雷是最常用的)作用于P2Y受体,并且常与乙酰水杨酸(ASA)联合使用。评估了六种噻吩并[2,3-b]吡啶的体外抗血小板活性;所有衍生物均对血小板活化和聚集有作用,并与ASA表现出协同作用。与氯吡格雷相比,一些化合物表现出更强的活性。因此,这些化合物代表了用于改善患者治疗的潜在新型P2Y抑制剂。