Show simple item record

dc.contributor.authorEra B.
dc.contributor.authorDelogu G.L.
dc.contributor.authorPintus F.
dc.contributor.authorFais A.
dc.contributor.authorGatto G.
dc.contributor.authorUriarte E.
dc.contributor.authorBorges F.
dc.contributor.authorKumar A.
dc.contributor.authorMatos M.J.
dc.date.accessioned2020-09-02T22:17:17Z
dc.date.available2020-09-02T22:17:17Z
dc.date.issued2020
dc.identifier10.1016/j.ijbiomac.2020.06.152
dc.identifier.citation162, , 774-780
dc.identifier.issn01418130
dc.identifier.urihttps://hdl.handle.net/20.500.12728/4379
dc.descriptionOverproduction of uric acid in the body leads to hyperuricemia, which is also closely related to gout. Uric acid production can be lowered by xanthine oxidase (XO) inhibitors. Inhibition of XO has also been proposed as a mechanism for improving cardiovascular health. Therefore, the search for new efficient XO inhibitors is an interesting topic in drug discovery. 3-Phenylcoumarins and 2-phenylbenzofurans are privileged scaffolds in medicinal chemistry. Their structural similarity makes them interesting molecules for a comparative study. Methoxy and nitro substituents were introduced in both scaffolds. The current study gives some insights into the synthesis and biological activity of these molecules against this important target. For the best compound of the series, the 3-(4-methoxyphenyl)-6-nitrocoumarin (4), the IC50 value, type of inhibition, cytotoxicity on B16F10 cells and ADME theoretical properties, were determined. Docking studies were also performed in order to better understand the interactions of this molecule with the XO binding pocket. This work is a preliminary screening for further design and synthesis of new non-purinergic derivatives as potential compounds involved in the inflammatory suppression, specially related to gout. © 2020 Elsevier B.V.
dc.language.isoen
dc.publisherElsevier B.V.
dc.subject2-Phenylbenzofurans
dc.subject3-Phenylcoumarins
dc.subjectXanthine oxidase inhibitors
dc.subject2 hydroxybenzylalcohol derivative
dc.subject2 hydroxybenzyltriphenylphosphonium bromide
dc.subject2 phenylbenzofuran
dc.subject2 phenylbenzofuran derivative
dc.subject3 arylcoumarin derivative
dc.subject3 phenylcoumarin derivative
dc.subjectallopurinol
dc.subjectbenzofuran derivative
dc.subjectcoumarin derivative
dc.subjectfebuxostat
dc.subjectunclassified drug
dc.subjectxanthine oxidase
dc.subjectxanthine oxidase inhibitor
dc.subjectanimal cell
dc.subjectArticle
dc.subjectchromatography
dc.subjectconcentration (parameter)
dc.subjectcontrolled study
dc.subjectcytotoxicity
dc.subjectdrug receptor binding
dc.subjectenzyme inhibition
dc.subjectevaporation
dc.subjectIC50
dc.subjectmolecular docking
dc.subjectmouse
dc.subjectnonhuman
dc.subjectparticle size
dc.subjectphysical chemistry
dc.subjectthin layer chromatography
dc.titleLooking for new xanthine oxidase inhibitors: 3-Phenylcoumarins versus 2-phenylbenzofurans
dc.typeArticle


Files in this item

Thumbnail

This item appears in the following Collection(s)

Show simple item record