当前位置: X-MOL 学术Eur. J. Med. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Thieno[2,3-b]pyridine derivatives are potent anti-platelet drugs, inhibiting platelet activation, aggregation and showing synergy with aspirin
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2017-11-07 , DOI: 10.1016/j.ejmech.2017.11.014
Naif K. Binsaleh , Catherine A. Wigley , Kathryn A. Whitehead , Michelle van Rensburg , Johannes Reynisson , Lisa I. Pilkington , David Barker , Sarah Jones , Nina C. Dempsey-Hibbert

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 P2Y12 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 P2Y12 inhibitors for improved treatment for patients.



中文翻译:

噻吩并[2,3- b ]吡啶衍生物是有效的抗血小板药物,可抑制血小板活化,聚集并显示与阿司匹林的协同作用

抑制血小板功能的药物通常用于预防患有急性冠状动脉综合征(ACS)或有中风风险的患者的血凝块形成。噻吩并[3,2- c ]吡啶类治疗药物(最普遍使用的是氯吡格雷)靶向P2Y 12受体,并经常与乙酰水杨酸(ASA)结合使用。评估了六种噻吩并[2,3- b ]吡啶的体外抗血小板活性。所有衍生物均显示出对血小板活化和聚集的作用,并显示出与ASA的协同作用。与氯吡格雷相比,某些化合物具有更高的活性。因此,这些化合物代表了潜在的新型P2Y 12 抑制剂以改善患者的治疗。

更新日期:2017-11-07
down
wechat
bug