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Synthesis and Antithrombotic Effect of Xanthone Derivatives

1996; Oxford University Press; Volume: 48; Issue: 9 Linguagem: Inglês

10.1111/j.2042-7158.1996.tb05994.x

2042-7158

Chun‐Nan Lin, Hsin‐Kaw Hsieh, Shiou-Jyh Liou, Huey-Jiun Ko, Hsien‐Cheng Lin, Mei‐Ing Chung, Feng‐Nien Ko, Hongwen Liu, Che‐Ming Teng,

Synthesis of Organic Compounds

Abstract A series of xanthone derivatives was 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. 2-Prenyloxyxanthone showed the most potent inhibition of rabbit washed platelet aggregation induced by arachidonic acid (IC50 = 10.2 μM). Of the compounds tested in human PRP, 2-[3 (propylamino)-2-hydroxypropoxy]xanthone (4) hydrochloride salt exhibited the most potent inhibition of platelet aggregation induced by adrenaline (IC50 = 4.4 μM), whereas in evaluation of mouse antithrombotic activity, compound 4 exhibited the most potent protection of mice from thrombotic challenge. Compound 4, 2-[3-(isopropylamino)-2-hydroxypropoxylxanthone hydrochloride salt and 2,5 dihydroxyxanthone suppressed the secondary aggregation induced by adrenaline in human PRP. We conclude that the antiplatelet effects of these compounds are mainly due to an inhibitory effect on thromboxane formation.