Synthesis and Antithrombotic Effect of Xanthone Derivatives

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 (1C50 = 10.2 microM). 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 microM), 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.

Synthesis, biological evaluation, and molecular docking study of 3-(3′-heteroatom substituted-2′-hydroxy-1′-propyloxy) xanthone analogues as novel topoisomerase IIα catalytic inhibitor

“…Xanthones have a diverse biological profile including antihypertensive [2], anticonvulsant [3], anti-thrombotic [4], anticholinesterase [5], and anti-cancer activities [6,7], which depend on their wide range of structures modified by substituents on the xanthone ring. The simple structural scaffold and diverse pharmacological properties of xanthone derivatives have prompted many scientists to isolate these compounds from natural resources or synthesize them as novel drug candidates.…”

One-step synthesis of 2-pentanone from ethanol over K-Pd/MnOx-ZrO2-ZnO catalyst

“…It is evident that the K-Pd/MnO x -ZrO 2 -ZnO catalyst adsorbs CO 2 and NH 3 , thus possesses both acidic and basic properties. The basic, acid and metal sites are required for aldol, dehydration and hydrogenation reaction, respectively [12].…”

“…Various supported metal catalysts have recently been described which can be utilized in the one-step synthesis of methyl isobutyl ketone (MIBK) from acetone. These include Ni supported on MgO [9], ALPON [10], or Al 2 O 3 [11], Pd-on-MgO promoted by Na [12], Pt-HMFI [13] and Pd or Ni supported on Mg/Al hydrotalcite [14]. Herein, we disclose a first report on the heterogeneous one-step synthesis of 2-pentanone from readily available ethanol over K-Pd/MnO x -ZrO 2 -ZnO catalyst.…”

Synthesis and Evaluation of Some Xanthone Derivatives for Anti‐Arrhythmic, Hypotensive Properties and Their Affinity for Adrenergic Receptors

“…Depending on the kind and place of substitution in one of the xanthone rings e. g., antitumor [14,15], anti-inflammatory [16], antitrombotic [17], antituberculotic [18], anticonvulsant [19,20], neuropharmacological [21,22], modulatory activity of protein kinase C [23], and antihypertensive [24,25] effects were described.…”