ω-氨基烷氧基呫吨酮的合成及其抗血小板作用
Synthesis and antiplatelet effects of omega-aminoalkoxylxanthones.
作者信息
Lin C N, Liou S S, Lai S C, Lin H C, Ko F N, Liu H W, Teng C M
机构信息
School of Pharmacy, Kaohsuing Medical College, Taiwan, ROC.
出版信息
J Pharm Pharmacol. 1995 Jul;47(7):588-94. doi: 10.1111/j.2042-7158.1995.tb06720.x.
A series of omega-aminoalkoxylxanthones were synthesized and tested in-vitro for their ability to inhibit aggregation of rabbit washed platelets and human platelet-rich plasma (PRP) induced by various inducers. Nine of these compounds showed more potent antiplatelet effects than natural norathyriol tetraacetate on collagen-induced aggregation. The various omega-aminoalkoxyl side chains of the synthesized compounds modified the antiplatelet effects. All the compounds tested in human PRP showed significant inhibition of secondary aggregation induced by adrenaline, suggesting that the antiplatelet effects of these compounds is mainly due to an inhibitory effect on thromboxane formation. These compounds at high concentration also cause vasorelaxing action in rat thoracic aorta.
合成了一系列ω-氨基烷氧基呫吨酮，并在体外测试了它们抑制由各种诱导剂诱导的兔洗涤血小板和人富血小板血浆（PRP）聚集的能力。其中九种化合物在抑制胶原诱导的聚集方面显示出比天然去甲氧基呫吨酮四乙酸酯更强的抗血小板作用。合成化合物的各种ω-氨基烷氧基侧链改变了抗血小板作用。在人PRP中测试的所有化合物均显示出对肾上腺素诱导的二次聚集有显著抑制作用，表明这些化合物的抗血小板作用主要是由于对血栓素形成的抑制作用。这些化合物在高浓度时也会引起大鼠胸主动脉的血管舒张作用。
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