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

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。

A series of carbamate-isosorbide-3-n-butylphthalide ring opening derivative trihybrids（8a-8i） were synthesized, and their structures were confirmed by I H 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 aggre- gation activity and aqueous solubility. Therefore, compound 8i may he a potential platelet aggregation inhibitor for further investigation.