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Title: 2-Styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study
Authors: Fernandes, Eduarda
Carvalho, Félix
Silva, Artur
Santos, Clementina M.M.
Pinto, Diana
Cavaleiro, José
Bastos, Maria de Lourdes
Keywords: 2-Styrylchromones
Xanthine oxidase inhibition
Issue Date: 2002
Publisher: Taylor & Francis
Citation: Fernandes, Eduarda; Carvalho, Félix; Silva, Artur; Santos, Clementina; Pinto, Diana; Cavaleiro, José; Bastos, Maria de Lourdes (2002) - 2-Styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study. ISSN 1475-6366. 17:1, p. 45-48
Abstract: The purpose of this study was the evaluation of the xanthine oxidase (XO) inhibition produced by some synthetic 2-styrylchromones. Ten polyhydroxylated derivatives with several substitution patterns were synthesised, and these and a positive control, allopurinol, were tested for their effects on XO activity by measuring the formation of uric acid from xanthine. The synthesised 2-styrylchromones inhibited xanthine oxidase in a concentration-dependent and non-competitive manner. Some IC50 values found were as low as 0.55mM, which, by comparison with the IC50 found for allopurinol (5.43 mM), indicates promising new inhibitors. Those 2-styrylchromones found to be potent XO inhibitors should be further evaluated as potential agents for the treatment of pathologies related to the enzyme’s activity, as is the case of gout, ischaemia/ reperfusion damage, hypertension, hepatitis and cancer.
Peer review: yes
ISSN: 1475-6366
Appears in Collections:PTV - Artigos em Revistas Indexados ao ISI/Scopus

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