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Synthesis and antithrombotic effect of xanthone derivatives
1School of Pharmacy, Department of Internal Medicine, Kaohsiung Medical College, Taiwan, R.O.C.
The Journal of Pharmacy and Pharmacology
|September 1, 1996
Summary
New xanthone derivatives show potent antiplatelet activity. These compounds inhibit platelet aggregation and offer protection against thrombosis, primarily by reducing thromboxane formation.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Biochemistry
Background:
- Platelet aggregation plays a crucial role in thrombotic events.
- Xanthone derivatives are being explored for their potential therapeutic properties.
Purpose of the Study:
- To synthesize and evaluate xanthone derivatives for antiplatelet and antithrombotic activities.
- To identify specific xanthone compounds with potent inhibitory effects on platelet aggregation.
Main Methods:
- In-vitro synthesis and testing of xanthone derivatives.
- Assessment of inhibition of rabbit washed platelet and human platelet-rich plasma (PRP) aggregation induced by various agents.
- Evaluation of antithrombotic activity in a mouse model.
Main Results:
- 2-Prenyloxyxanthone demonstrated potent inhibition of arachidonic acid-induced rabbit platelet aggregation (IC50 = 10.2 microM).
- Compound 4 (2-[3-(propylamino)-2-hydroxypropoxy]xanthone hydrochloride salt) was most effective against adrenaline-induced human PRP aggregation (IC50 = 4.4 microM) and showed significant antithrombotic protection in mice.
- Compounds 4, 2-[3-(isopropylamino)-2-hydroxypropoxylxanthone hydrochloride salt, and 2,5 dihydroxyxanthone inhibited secondary aggregation in human PRP induced by adrenaline.
Conclusions:
- The synthesized xanthone derivatives exhibit significant antiplatelet and antithrombotic potential.
- The antiplatelet effects are primarily attributed to the inhibition of thromboxane formation.
- Specific compounds, notably compound 4, show promise for further development as antithrombotic agents.