The screening and characterization of 6-aminopurine-based xanthine oxidase inhibitors.
Basic Information
ID: ALA1143034
Journal: Bioorg Med Chem
Title: The screening and characterization of 6-aminopurine-based xanthine oxidase inhibitors.
Authors: Hsieh JF, Wu SH, Yang YL, Choong KF, Chen ST.
Abstract: Xanthine oxidase (XO) is a key enzyme which can catalyze xanthine to uric acid causing hyperuricemia in humans. By using the fractionation technique and inhibitory activity assay, an active compound that prevents XO from reacting with xanthine was isolated from wheat leaf. It was identified by the Mass and NMR as 6-aminopurine (adenine). A structure-activity study based on 6-aminopurine was conducted. The inhibition of XO activity by 6-aminopurine (IC(50)=10.89+/-0.13 microM) and its analogues was compared with that by allopurinol (IC(50)=7.82+/-0.12 microM). Among these analogues, 2-chloro-6(methylamino)purine (IC(50)=10.19+/-0.10 microM) and 4-aminopyrazolo[3,4-d] pyrimidine (IC(50)=30.26+/-0.23 microM) were found to be potent inhibitors of XO. Kinetics study showed that 2-chloro-6(methylamino)purine is non-competitive, while 4-aminopyrazolo[3,4-d]pyrimidine is competitive against XO.
CiteXplore: 17379526
DOI: 10.1016/j.bmc.2007.03.010
Patent ID: ┄