Abstract

Thongchai Khammee¹, Warakorn Jongsu¹, Mayuso Kuno² and Sunit Suksamrarn²

DOI : http://dx.doi.org/10.13005/ojc/340104

Gout is one of the most severe health problems of the aged and is caused by high levels of uric acid in the blood. The inhibition of Xanthine oxidase (XO) is one strategy to retain gout disease. Oxygenated xanthones and derivatives have been shown many important biological activities. However, some xanthones have the small amount of nature and its sulfur analogs, thioxanthone has not been well studied in their bioactivity. A series of hydroxyxanthones and allylxanthones analogous 3-5 have been synthesized and screened for their anti-XO activity. Leads to the discovery of 2,4-diallyl-1,3-dihydroxythioxanthone (5b) as the most active inhibitor with IC₅₀ = 0.69±0.02 mM. Consequent molecular docking analysis by AutoDock 4.2 indicated that the most active compound (5b) inhibits XO by accommodated at the binding site of XO.

Xanthine Oxidase Inhibitors; Xanthone; Thioxanthone; Molecular Docking

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