2-styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study

• Type: Article in International Scientific Journal
• Date: 2002

Authors

Fernandes, E (Author) FFUP; Carvalho, F (Author) FFUP; Silva, AMS (Author) Other; Santos, CMM (Author) Other; Pinto, DCGA (Author) Other; Cavaleiro, JAS (Author) Other; Bastos, MD (Author) FFUP

Journal

Title: Journal of Enzyme Inhibition and Medicinal Chemistry

Vol. 17

Pages: 45-48

ISSN: 1475-6366

Publisher: Taylor & Francis

Indexing

ISI Web of Knowledge - 31 Citations

Scopus - 38 Citations

Scientific classification

FOS: Medical and Health sciences > Basic medicine

Other information

Authenticus ID: P-000-QFM

DOI: 10.1080/14756360290019944

Abstract (EN): 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 IC(50) values found were as low as 0.55 muM, which, by comparison with the IC(50) found for allopurinol (5.43 muM), 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.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 4