Lin Kai-Wei, Fang Song-Chwan, Hung Chi-Feng, Shieh Bor-Jinn, Yang Shyh-Chyun, Teng Che-Ming, Lin Chun-Nan
School of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan.
Arch Pharm (Weinheim). 2009 Jan;342(1):19-26. doi: 10.1002/ardp.200800002.
A series of omega-aminoalkoxylxanthones was synthesized and tested in vitro for their ability to inhibit platelet aggregation and cause vasorelaxing action. Compounds 4, 5, 12, 17, and 18 showed significant antiplatelet effects on thrombin-, arachidonic acid (AA)-, collagen-, and platelet activating factor (PAF)-induced washed rabbit platelet aggregation and exhibited inhibition of primary and secondary aggregation induced by adenosine-5'-diphosphate (ADP) in human platelet-rich-plasma (PRP). Compounds 4, 17, and 18 revealed vasorelaxing activities in rat thoracic aorta. We concluded that these compounds may be developed as new antithrombotic agents.
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血小板聚集和引起血管舒张作用的能力。化合物4、5、12、17和18对凝血酶、花生四烯酸（AA）、胶原蛋白和血小板活化因子（PAF）诱导的洗涤兔血小板聚集显示出显著的抗血小板作用，并对富含人血小板血浆（PRP）中由5'-二磷酸腺苷（ADP）诱导的初级和次级聚集表现出抑制作用。化合物4、17和18在大鼠胸主动脉中显示出血管舒张活性。我们得出结论，这些化合物可能被开发为新型抗血栓药物。
