[苯丙酰胺抗血小板聚集化合物的设计、合成和生物学评价]。

药学学报 Pub Date : 2017-01-01

Yu Yang, Jian Zuo, Jia-ming Li, Xiao-dong Ma, Yan-chun Zhang, Wei-jun Huang

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引用次数: 0

摘要

采用药物载体组合策略，设计合成了20个结构新颖的苯丙酰胺类似物。通过IR、1H NMR、13C NMR和MS对目标化合物的结构进行了鉴定，并通过Bron法对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进行了生物学评价。结果表明，化合物6b、9b、9d和9h对AA诱导的血小板聚集具有较强的抑制作用。同时，化合物6b、6d、6j、9b和9g对ADP诱导的血小板聚集有明显抑制作用。

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本刊更多论文

[Design, synthesis, and biological evaluation of phenylpropenamides compounds as anti-platelet aggregation].

Twenty phenylpropenamide analogs with structural novelty were designed and synthesized upon pharmacophore-combination strategy. The structures of target compounds were elucidated by IR, 1H NMR, 13C NMR and MS, and all the target compounds were biologically evaluated for the inhibitory activities of platelet aggregation induced by adenosine diphoshate（ADP） and（AA） arachidonic acid via Bron method. As a result, compounds 6b, 9b, 9d and 9h demonstrated potent inhibitory activity against platelet aggregation induced by AA. Meanwhile, compounds 6b, 6d, 6j, 9b and 9g exhibited significant suppression of platelet aggregation induced by ADP.

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来源期刊

药学学报 Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)

CiteScore

1.20

自引率

0.00%

发文量

期刊介绍： Acta Pharmaceutica Sinica B (APSB) is a bimonthly English peer-reviewed online journal in ScienceDirect, which publishes significant original research articles, communications and high quality reviews of recent advances. APSB encourages submissions from all areas of pharmaceutical sciences, including pharmacology, pharmaceutics, medicinal chemistry, natural products, pharmacognosy, pharmaceutical analysis and pharmacokinetics. APSB is a part of the series Acta Pharmaceutica Sinica, which was founded in 1953. The journal is co-published by Elsevier B.V., in association with the Institute of MateriaMedica, Chinese Academy of Medical Sciences and Chinese Pharmaceutical Association.