Wang Chaoqing, Wang Yan, Deng Qingsong, Liu Xiujie
School of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, China.
Tianjin Key Laboratory of Organic Solar Cells and Photochemical Conversion, School of Chemistry and.
Iran J Pharm Res. 2019 Fall;18(4):1803-1815. doi: 10.22037/ijpr.2019.1100856.
In our present investigation, a series of novel 4-methoxy-1,3-benzenediolyl-hydrazones were designed and synthesized, and their ability to inhibit platelet aggregation was evaluated by adenosine diphosphate (ADP) and arachidonic acid (AA). The structures of the synthesized compounds were confirmed by spectral data. Results demonstrated that the activities of all compounds excelled the positive drug Picotamide (25.1% inhibition rate) and seven compounds (, , , , , , ) have efficiently inhibited platelet aggregation even higher than Clopidogrel (37.6% inhibition rate) induced by AA. Among them, (39.8% inhibition rate was considered as the most potent analogue. Evaluation of cytotoxic activity of the compounds against L929 cell line revealed that none of the compounds have significant cytotoxicity. Thus, diolylhydrazones derives are potential to be antiplatelet aggregation inhibitors and maybe working in AA-induced selectively.
在我们目前的研究中,设计并合成了一系列新型的4-甲氧基-1,3-苯二酚腙,并通过二磷酸腺苷(ADP)和花生四烯酸(AA)评估了它们抑制血小板聚集的能力。通过光谱数据确认了合成化合物的结构。结果表明,所有化合物的活性均优于阳性药物匹可托胺(抑制率25.1%),并且七种化合物(,,,,,,)对AA诱导的血小板聚集的抑制效果甚至高于氯吡格雷(抑制率37.6%)。其中,(抑制率39.8%)被认为是最有效的类似物。对这些化合物针对L929细胞系的细胞毒性活性评估表明,没有一种化合物具有显著的细胞毒性。因此,二酚腙衍生物有潜力成为抗血小板聚集抑制剂,并且可能在AA诱导的过程中具有选择性作用。