Basic Information
ID: ALA3745646
Journal: Bioorg Med Chem
Title: 9-Benzoyl 9-deazaguanines as potent xanthine oxidase inhibitors.
Authors: Rodrigues MV, Barbosa AF, da Silva JF, dos Santos DA, Vanzolini KL, de Moraes MC, Corrêa AG, Cass QB.
Abstract: A novel potent xanthine oxidase inhibitor, 3-nitrobenzoyl 9-deazaguanine (LSPN451), was selected from a series of 10 synthetic derivatives. The enzymatic assays were carried out using an on-flow bidimensional liquid chromatography (2D LC) system, which allowed the screening¸ the measurement of the kinetic inhibition constant and the characterization of the inhibition mode. This compound showed a non-competitive inhibition mechanism with more affinity for the enzyme-substrate complex than for the free enzyme, and inhibition constant of 55.1±9.80 nM, about thirty times more potent than allopurinol. Further details of synthesis and enzymatic studies are presented herein.
CiteXplore: 26712096
DOI: 10.1016/j.bmc.2015.12.006
Patent ID: ┄
Associated Items: Associated Bioactivities Associated Assays Associated Compounds Associated Targets