川芎嗪四氢异喹啉类化合物的设计、合成及其抗血小板聚集活性

Design, synthesis and anti-platelet aggregation activities of ligustrazine-tetrahydroisoquinoline derivatives

摘要: 运用药物化学中的拼合原理, 设计合成了15个新型川芎嗪四氢异喹啉类化合物, 其结构经IR、NMR、ESI-MS确证。采用Bron比浊法测定了川芎嗪四氢异喹啉类化合物对二磷酸腺苷 (adenosine diphosphate, ADP) 及花生四烯酸 (arachidonic acid, AA) 诱导的血小板聚集的抑制活性。初步药理结果显示, 化合物7g、7h和7n对AA诱导的血小板聚集具有较好的抑制作用; 化合物7o对ADP诱导的血小板聚集具有较好的抑制作用。

Abstract: Fifteen novel ligustrazine-tetrahydroisoquinoline derivatives were designed and synthesized according to the association principle of pharmaceutical chemistry. The structures were identified by IR, NMR and ESI-MS. The inhibitory activities of platelet aggregation induced by ADP and AA have been measured by Bron method. Preliminary pharmacological results showed that compounds 7g, 7h and 7n had potent inhibitory activity against platelet aggregation induced by AA, and the compound 7o showed significant inhibitory activity against platelet aggregation induced by ADP.