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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

9-Benzoyl 9-deazaguanines as potent xanthine oxidase inhibitors

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Rodrigues, Marili V. N. [1, 2] ; Barbosa, Alexandre F. [3] ; da Silva, Julia F. [3] ; dos Santos, Deborah A. [3] ; Vanzolini, Kenia L. [2] ; de Moraes, Marcela C. [2, 4] ; Correa, Arlene G. [3] ; Cass, Quezia B. [2]
Total Authors: 8
[1] Univ Estadual Campinas, Ctr Pluridisciplinar Pesquisas Quim Biol & Agr, BR-13148218 Paulinia, SP - Brazil
[2] Univ Fed Sao Carlos, Dept Quim, SEPARARE Nucleo Pesquisa Cromatog, BR-13565905 Sao Carlos, SP - Brazil
[3] Univ Fed Sao Carlos, Dept Quim, Lab Sintese Prod Nat, BR-13565905 Sao Carlos, SP - Brazil
[4] Univ Fed Fluminense, Inst Quim, Dept Quim Organ, BR-24020141 Niteroi, RJ - Brazil
Total Affiliations: 4
Document type: Journal article
Source: Bioorganic & Medicinal Chemistry; v. 24, n. 2, p. 226-231, JAN 15 2016.
Web of Science Citations: 11

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. (AU)

FAPESP's process: 13/01710-1 - Enzyme ligand: new models of screening
Grantee:Quezia Bezerra Cass
Support type: Research Projects - Thematic Grants
FAPESP's process: 13/07600-3 - CIBFar - Center for Innovation in Biodiversity and Drug Discovery
Grantee:Glaucius Oliva
Support type: Research Grants - Research, Innovation and Dissemination Centers - RIDC
FAPESP's process: 13/50680-8 - Quinoxaline derivatives as antiparasitic drugs: proof of concept
Grantee:Arlene Gonçalves Corrêa
Support type: Research Grants - Research Partnership for Technological Innovation - PITE