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Synthesis and Vasorelaxant and Platelet Antiaggregatory Activities of a New Series of 6-Halo-3-phenylcoumarins

机译:一系列新的6-卤代-3-苯基香豆素的合成血管舒张剂和血小板的抗聚集活性

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摘要

A series of 6-halo-3-hydroxyphenylcoumarins (resveratrol-coumarins hybrid derivatives) was synthesized in good yields by a Perkin reaction followed by hydrolysis. The new compounds were evaluated for their vasorelaxant activity in intact rat aorta rings pre-contracted with phenylephrine (PE), as well as for their inhibitory effects on platelet aggregation induced by thrombin in washed human platelets. These compounds concentration-dependently relaxed vascular smooth muscle and some of them showed a platelet antiaggregatory activity that was up to thirty times higher than that shown by trans-resveratrol and some other previously synthesized derivatives.
机译:通过珀金反应然后水解,以高收率合成了一系列6-卤-3-羟基苯基香豆素(白藜芦醇-香豆素杂化衍生物)。评估了新化合物在与去氧肾上腺素(PE)预收缩的完整大鼠主动脉环中的血管舒张活性,以及​​对凝血酶诱导的血小板聚集在洗涤后的人血小板中的抑制作用。这些化合物的浓度依赖性地松弛血管平滑肌,其中一些显示出抗血小板聚集活性,该活性比反式白藜芦醇和其他一些先前合成的衍生物高出三十倍。

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