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川芎嗪 - 四氢异喹啉衍生物的设计、合成及抗血小板聚集活性

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

作者信息

Xie Di, Zhang En-li, Li Jia-ming, Wang Jie, He Guang-wei

出版信息

Yao Xue Xue Bao. 2015 Mar;50(3):326-31.

Abstract

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.

摘要

摘要

根据药物化学的拼合原理设计并合成了15个新型川芎嗪-四氢异喹啉衍生物。通过红外光谱(IR)、核磁共振(NMR)和电喷雾电离质谱(ESI-MS)对其结构进行了鉴定。采用比浊法测定了这些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。初步药理结果表明,化合物7g、7h和7n对AA诱导的血小板聚集具有较强的抑制活性,化合物7o对ADP诱导的血小板聚集具有显著的抑制活性。

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