Synthesis of Novel 3-Butylphthalide Derivatives Containing Isopentenylphenol Moiety as Potential Antiplatelet Agents for the Treatment of Ischemic Stroke,Chemistry & Biodiversity

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Synthesis of Novel 3-Butylphthalide Derivatives Containing Isopentenylphenol Moiety as Potential Antiplatelet Agents for the Treatment of Ischemic Stroke
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2022-11-24 , DOI: 10.1002/cbdv.202201002
Qinyang Yu ₁ , Bilan Luo ₁ , Zhongfu Luo ₁ , Xu Zhong ₁ , Yi Li ₁ , Yi Zhang ₁ , Gaofeng Zhu ₁ , Bing Guo ₁ , Lei Tang ₁ , Yong Li ₁ , Lingling Fan ₁

Affiliation

In order to find novel antiplatelet drugs for the treatment of ischemic stroke, a series of 3-butylphthalide derivatives containing isopentenylphenol moiety were designed, synthesized and characterized with spectroscopic analyses. The in vitro antiplatelet activity results indicated that compound 3 better inhibited the arachidonic acid (AA) induced platelet aggregation than aspirin (ASP) and 3-butylphthalide (NBP). Additionally, compared with precursor NBP, compound 3 possessed outstanding antithrombotic activity in the animal experiment model, which could effectively alleviate the formation of tail thrombus and carotid artery thrombus in mice. More importantly, intraperitoneal administration of compound 3 can well protected the rats against ischemia/reperfusion-induced brain injury. Further pharmacokinetic (PK) assay indicated that compound 3 had good absorption characteristics and metabolic stability in vivo. Overall, the present research provides a new candidate compound for the treatment of ischemic stroke caused by platelet aggregation.

中文翻译：

含有异戊烯基苯酚部分的新型 3-丁基苯酞衍生物的合成作为治疗缺血性中风的潜在抗血小板药物

为了寻找治疗缺血性中风的新型抗血小板药物，设计、合成了一系列含有异戊烯基苯酚基团的 3-丁基苯酞衍生物，并用光谱分析对其进行了表征。体外抗血小板活性结果表明化合物3比阿司匹林 (ASP) 和 3-丁基苯酞 (NBP) 更好地抑制花生四烯酸 (AA) 诱导的血小板聚集。此外，与前体NBP相比，化合物 3在动物实验模型中具有突出的抗血栓形成活性，可有效缓解小鼠尾部血栓和颈动脉血栓的形成。更重要的是，化合物3的腹膜内给药能很好地保护大鼠免受缺血/再灌注引起的脑损伤。进一步的药代动力学 (PK) 测定表明化合物 3在体内具有良好的吸收特性和代谢稳定性。总的来说，本研究为治疗由血小板聚集引起的缺血性中风提供了一种新的候选化合物。

更新日期：2022-11-24

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