丹皮酚肟衍生物的设计、合成及抗血小板聚集活性
Design, synthesis and anti-platelet aggregation activity of paeonol oxime derivatives
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摘要: 以丹皮酚为起始原料，经结构修饰得到25个新的丹皮酚肟类衍生物4a ~ 4y，其结构经过高分辨质谱、核磁共振氢谱确证。所合成的目标化合物对二磷酸腺苷（ADP）和胶原诱导的血小板聚集均具有一定的抑制活性，其中化合物4h、4j对两种诱导剂诱导的血小板聚集优于阳性对照药阿司匹林，且化合物4h具有较好的水溶性和类药性，可作为新的抗血小板活性化合物进一步研究。Abstract: In order to afford new antiplatelet agents with higher potency, a series of paeonol oxime derivatives (4a-4y) were designed and synthesized from paeonol.Their structures were confirmed by HRMS, 1H NMR spectra.The anti-platelet aggregation activity of the target compounds was evaluated.The results revealed that most of them had moderate to good anti-platelet aggregation activity.Among them, compound 4h and 4j were the most potent on adenosine diphosphate (ADP)-induced platelet aggregation and collagen-induced platelet aggregation. Furthermore, the target compound 4h not only showed strong antiplatelet aggregation activity, but also exhibited good water-solubility and drug-like properties, which can be used as a new antiplatelet active compound for further research.
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