Advanced search
Start date
Betweenand
Related content
(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

Full text
Author(s):
Rodrigues, Marili V. N. [1, 2] ; Barbosa, Alexandre F. [3] ; da Silva, Julia F. [3] ; dos Santos, Deborah A. [3] ; Vanzolini, Kenia L. [1] ; de Moraes, Marcela C. [1, 4] ; Correa, Arlene G. [3] ; Cass, Quezia B. [1]
Total Authors: 8
Affiliation:
[1] Univ Fed Sao Carlos, Dept Quim, SEPARARE Nucleo Pesquisa Cromatog, BR-13565905 Sao Carlos, SP - Brazil
[2] Univ Estadual Campinas, Ctr Pluridisciplinar Pesquisas Quim Biol & Agr, BR-13148218 Paulinia, 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
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. (AU)

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