异恶唑
血小板
化学
血小板活化
药理学
血小板聚集
分泌物
配体(生物化学)
IC50型
P-选择素
血小板聚集抑制剂
体外
生物化学
组合化学
立体化学
受体
医学
内科学
作者
Margarita Gutiérrez,Jessica Amigo,Eduardo Fuentes,Iván Palomo,Luís Astudillo
出处
期刊:Platelets
[Informa]
日期:2013-07-10
卷期号:25 (4): 234-238
被引量:13
标识
DOI:10.3109/09537104.2013.807335
摘要
Nine synthetic isoxazoles were evaluated as antiplatelet agents and studied the possible mechanism of more active compound. The initial screening was evaluating all compounds against platelet aggregation assays. The most active compound was isoxazole 8 showing an inhibition of platelet aggregation around 70%. In subsequent experiments, ADP and collagen were used as agonists to explore the possible inhibitory mechanisms of isoxazole 8 in platelet aggregation and secretion. We reported the effect of isoxazole 8 for reducing the expression of inflammatory markers, such as soluble CD40 ligand (sCD40L) and soluble P-selectin (sP-selectin), on activated platelets. Of this form, an inhibition of sCD40L and sP-selectin can prevent the onset of an atherosclerotic lesion.
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