2-Styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study

Detalhes bibliográficos
Autor(a) principal: Fernandes, Eduarda
Data de Publicação: 2002
Outros Autores: Carvalho, Félix, Silva, Artur, Santos, Clementina M.M., Pinto, Diana, Cavaleiro, José, Bastos, Maria de Lourdes
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10198/3931
Resumo: The purpose of this study was the evaluation of the xanthine oxidase (XO) inhibition produced by some synthetic 2-styrylchromones. Ten polyhydroxylated derivatives with several substitution patterns were synthesised, and these and a positive control, allopurinol, were tested for their effects on XO activity by measuring the formation of uric acid from xanthine. The synthesised 2-styrylchromones inhibited xanthine oxidase in a concentration-dependent and non-competitive manner. Some IC50 values found were as low as 0.55mM, which, by comparison with the IC50 found for allopurinol (5.43 mM), indicates promising new inhibitors. Those 2-styrylchromones found to be potent XO inhibitors should be further evaluated as potential agents for the treatment of pathologies related to the enzyme’s activity, as is the case of gout, ischaemia/ reperfusion damage, hypertension, hepatitis and cancer.
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spelling 2-Styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study2-StyrylchromonesAllopurinolBenzopyroneXanthine oxidase inhibitionThe purpose of this study was the evaluation of the xanthine oxidase (XO) inhibition produced by some synthetic 2-styrylchromones. Ten polyhydroxylated derivatives with several substitution patterns were synthesised, and these and a positive control, allopurinol, were tested for their effects on XO activity by measuring the formation of uric acid from xanthine. The synthesised 2-styrylchromones inhibited xanthine oxidase in a concentration-dependent and non-competitive manner. Some IC50 values found were as low as 0.55mM, which, by comparison with the IC50 found for allopurinol (5.43 mM), indicates promising new inhibitors. Those 2-styrylchromones found to be potent XO inhibitors should be further evaluated as potential agents for the treatment of pathologies related to the enzyme’s activity, as is the case of gout, ischaemia/ reperfusion damage, hypertension, hepatitis and cancer.Taylor & FrancisBiblioteca Digital do IPBFernandes, EduardaCarvalho, FélixSilva, ArturSantos, Clementina M.M.Pinto, DianaCavaleiro, JoséBastos, Maria de Lourdes2011-04-04T14:34:49Z20022002-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10198/3931engFernandes, Eduarda; Carvalho, Félix; Silva, Artur; Santos, Clementina; Pinto, Diana; Cavaleiro, José; Bastos, Maria de Lourdes (2002). 2-Styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study. ISSN 1475-6366. 17:1, p. 45-481475-636610.1080/14756360290019944info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2023-11-21T10:08:21Zoai:bibliotecadigital.ipb.pt:10198/3931Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T22:56:08.820247Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse
dc.title.none.fl_str_mv 2-Styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study
title 2-Styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study
spellingShingle 2-Styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study
Fernandes, Eduarda
2-Styrylchromones
Allopurinol
Benzopyrone
Xanthine oxidase inhibition
title_short 2-Styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study
title_full 2-Styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study
title_fullStr 2-Styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study
title_full_unstemmed 2-Styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study
title_sort 2-Styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study
author Fernandes, Eduarda
author_facet Fernandes, Eduarda
Carvalho, Félix
Silva, Artur
Santos, Clementina M.M.
Pinto, Diana
Cavaleiro, José
Bastos, Maria de Lourdes
author_role author
author2 Carvalho, Félix
Silva, Artur
Santos, Clementina M.M.
Pinto, Diana
Cavaleiro, José
Bastos, Maria de Lourdes
author2_role author
author
author
author
author
author
dc.contributor.none.fl_str_mv Biblioteca Digital do IPB
dc.contributor.author.fl_str_mv Fernandes, Eduarda
Carvalho, Félix
Silva, Artur
Santos, Clementina M.M.
Pinto, Diana
Cavaleiro, José
Bastos, Maria de Lourdes
dc.subject.por.fl_str_mv 2-Styrylchromones
Allopurinol
Benzopyrone
Xanthine oxidase inhibition
topic 2-Styrylchromones
Allopurinol
Benzopyrone
Xanthine oxidase inhibition
description The purpose of this study was the evaluation of the xanthine oxidase (XO) inhibition produced by some synthetic 2-styrylchromones. Ten polyhydroxylated derivatives with several substitution patterns were synthesised, and these and a positive control, allopurinol, were tested for their effects on XO activity by measuring the formation of uric acid from xanthine. The synthesised 2-styrylchromones inhibited xanthine oxidase in a concentration-dependent and non-competitive manner. Some IC50 values found were as low as 0.55mM, which, by comparison with the IC50 found for allopurinol (5.43 mM), indicates promising new inhibitors. Those 2-styrylchromones found to be potent XO inhibitors should be further evaluated as potential agents for the treatment of pathologies related to the enzyme’s activity, as is the case of gout, ischaemia/ reperfusion damage, hypertension, hepatitis and cancer.
publishDate 2002
dc.date.none.fl_str_mv 2002
2002-01-01T00:00:00Z
2011-04-04T14:34:49Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://hdl.handle.net/10198/3931
url http://hdl.handle.net/10198/3931
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Fernandes, Eduarda; Carvalho, Félix; Silva, Artur; Santos, Clementina; Pinto, Diana; Cavaleiro, José; Bastos, Maria de Lourdes (2002). 2-Styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study. ISSN 1475-6366. 17:1, p. 45-48
1475-6366
10.1080/14756360290019944
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Taylor & Francis
publisher.none.fl_str_mv Taylor & Francis
dc.source.none.fl_str_mv reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron:RCAAP
instname_str Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron_str RCAAP
institution RCAAP
reponame_str Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
collection Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
repository.name.fl_str_mv Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
repository.mail.fl_str_mv
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