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丹参酮 IIA 衍生物的设计、合成与血管舒张活性。

Design, synthesis and vasodilative activity of tanshinone IIA derivatives.

机构信息

School of Pharmaceutical Science, Zhengzhou University, Zhengzhou, PR China.

出版信息

Bioorg Med Chem Lett. 2012 Aug 1;22(15):5141-3. doi: 10.1016/j.bmcl.2012.05.014. Epub 2012 Jun 16.

Abstract

A new series of tanshinone IIA (DIIA) derivatives were synthesized through the reaction of brominated tanshinone IIA (1-Br DIIA) and aromatic acids in the presence of K(2)CO(3). Twenty compounds were synthesized, and all of them were novel. Vasodilative activities for synthesized compounds were valuated in vitro on the contractile response of vascular thoracic aorta smooth muscle from Wistar rats. The results showed that most compounds exhibited a concentration-dependent inhibition on the contractile response of norepinephrine. Four prepared compounds, 4, 5, 8 and 13 revealed relatively remarkable vasodilative activity.

摘要

通过溴代丹参酮 IIA(1-Br DIIA)与芳香酸在 K2CO3 存在下的反应,合成了一系列新的丹参酮 IIA(DIIA)衍生物。合成了 20 种化合物,它们都是新型化合物。在 Wistar 大鼠胸主动脉平滑肌的收缩反应上,对合成化合物的血管舒张活性进行了体外评估。结果表明,大多数化合物对去甲肾上腺素的收缩反应具有浓度依赖性抑制作用。4、5、8 和 13 四个制备的化合物表现出相对显著的血管舒张活性。

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