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Allylxanthone Derivatives as Xanthine Oxidase Inhibitors : Synthesis , Biological Evaluation and Molecular Docking Study
| Content Provider | Semantic Scholar |
|---|---|
| Author | Khammee, Thongchai Kuno, Mayuso Suksamrarn, Sunit |
| Copyright Year | 2018 |
| Abstract | 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 Xanthine oxidase. |
| File Format | PDF HTM / HTML |
| Alternate Webpage(s) | http://www.orientjchem.org/download/43603/ |
| Language | English |
| Access Restriction | Open |
| Subject Keyword | Analog AutoDock Boat dock Docking (molecular) Gout Inhibitory Concentration 50 OLPC XO Projection screen Uric Acid Xanthine Oxidase Xanthones thioxanthone xanthone-containing compound biosynthetic process |
| Content Type | Text |
| Resource Type | Article |
