氨基甲酸酯-异山梨醇-丁苯酞开环物三联体的合成及抗血小板聚集活性

Synthesis and evaluation of carbamate-isosorbide-3-n-butylphthalide ring opening derivative trihybrids as novel platelet aggregation inhibitors

摘要: 合成一系列氨基甲酸酯-异山梨醇-丁苯酞开环物三联体( 8a ~ 8i) ，其结构经波谱确证；采用Born氏比浊法检测目标化合物对二磷酸腺苷(ADP)诱导的血小板聚集的抑制活性。结果表明，化合物 8i 对ADP诱导的血小板聚集抑制活性及水溶性均显著优于丁苯酞，具有深入研究价值。

Abstract: A series of carbamate-isosorbide-3-n-butylphthalide ring opening derivative trihybrids( 8a - 8i) were synthesized, and their structures were confirmed by ¹H NMR and MS. The inhibitory activity of the target compounds against adenosine diphosphate(ADP)-induced platelet aggregation was evaluated in vitro by Born′s turbidimetric assay. In comparison with 3-n-butylphthalide(NBP), compound 8i possessed better antiplatelet aggregation activity and aqueous solubility. Therefore, compound 8i may be a potential platelet aggregation inhibitor for further investigation.