硫化氢供体型丁苯酞开环衍生物的设计、合成及抗血小板活性

Design, synthesis and evaluation of hydrogen sulfide-releasing derivatives of ring opening 3-n-butylphthalide as novel platelet aggregation inhibitors

摘要: 设计合成了一系列硫化氢供体型丁苯酞开环衍生物( 5a ~ 5f )，其结构经质谱和核磁共振氢谱确证；采用Born氏比浊法检测目标化合物对二磷酸腺苷(ADP)和花生四烯酸(AA)诱导的血小板聚集的抑制活性，结果表明，化合物 5e 对ADP和AA诱导的血小板聚集抑制活性均显著优于丁苯酞，具有深入研究价值。

Abstract: A series of hydrogen sulfide-releasing derivatives of open ring 3-n-butylphthalide( 5a - 5f )were designed, synthesized, and their structures were confirmed by MS and ¹H NMR. The inhibitory activity of the target compounds against adenosine diphosphate(ADP)and arachidonic acid(AA)-induced platelet aggregation was evaluated in vitro by Born′s turbidimetric assay. In comparison with 3-n-butylphthalide(NBP), compound 5e possessed better antiplatelet aggregation activity. Therefore, it may be utilized as a lead compound for further investigation.