Chemistry Department, Faculty of Sciences, University Porto, 4169-007 Porto, Portugal.
Molecules. 2010 Jan 12;15(1):270-9. doi: 10.3390/molecules15010270.
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.
通过珀金反应和水解反应，我们成功地以较高产率合成了一系列 6-卤代-3-羟基苯基香豆素（白藜芦醇-香豆素杂合衍生物）。我们评估了这些新化合物对预先用苯肾上腺素（PE）收缩的完整大鼠主动脉环的血管舒张活性，以及对凝血酶诱导的人血小板聚集的抑制作用。这些化合物浓度依赖性地松弛血管平滑肌，其中一些化合物表现出的血小板抗聚集活性比反式白藜芦醇和其他一些先前合成的衍生物高三十倍。
