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Type: Artigo de periódico
Title: 9-benzoyl 9-deazaguanines As Potent Xanthine Oxidase Inhibitors
Author: Rodrigues
Marili V. N.; Barbosa
Alexandre F.; da Silva
Julia F.; dos Santos
Deborah A.; Vanzolini
Kenia L.; de Moraes
Marcela C.; Correa
Arlene G.; Cass
Quezia B.
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. (c) 2015 Elsevier Ltd. All rights reserved.
Subject: Purine Nucleoside Phosphorylase
9-deazapurine Derivatives
Country: OXFORD
Rights: embargo
Identifier DOI: 10.1016/j.bmc.2015.12.006
Date Issue: 2016
Appears in Collections:Unicamp - Artigos e Outros Documentos

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