Effect of mesoionic 4-phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2-phenylamine chloride derivative salts on the activities of the nitric oxide synthase and arginase of Leishmania amazonensis

Detalhes bibliográficos
Autor(a) principal: Bezerra, Rômulo José Soares
Data de Publicação: 2008
Outros Autores: Silva, Edson F. da, Echevarria, Aurea, Silva, Liliane Gomes da, Finkelstein, Léa Cysne, Monteiro, Fabiane Pereira, Leon, Leonor L., Genestra, Marcelo
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/32444
Resumo: Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunologia. Rio de Janeiro, RJ. Brasil.
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spelling Bezerra, Rômulo José SoaresSilva, Edson F. daEchevarria, AureaSilva, Liliane Gomes daFinkelstein, Léa CysneMonteiro, Fabiane PereiraLeon, Leonor L.Genestra, Marcelo2019-04-11T10:45:58Z2019-04-11T10:45:58Z2008BEZERRA, Rômulo José Soares et al. Effect of mesoionic 4-phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2- phenylamine chloride derivative salts on the activities of the nitric oxide synthase and arginase of Leishmania amazonensis. Journal of Enzyme Inhibition and Medicinal Chemistry, v. 23, n. 3, p. 328–333, June 2008.1475-6366https://www.arca.fiocruz.br/handle/icict/3244410.1080/147563607015856191475-6374engTaylor & FrancisLeishmania amazonensisÓxido NítricoLeishmania amazonensisMesionic compoundsPhenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2-phenylamineNitric oxideNitric oxide synthaseArginaseÓxido Nítrico SintaseArginaseEffect of mesoionic 4-phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2-phenylamine chloride derivative salts on the activities of the nitric oxide synthase and arginase of Leishmania amazonensisinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunologia. Rio de Janeiro, RJ. Brasil.Universidade Federal Rural do Rio de Janeiro. Departamento de Química. Seropédica, RJ, Brasil.Universidade Federal Rural do Rio de Janeiro. Departamento de Química. Seropédica, RJ, Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunologia. Rio de Janeiro, RJ. Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunologia. Rio de Janeiro, RJ. Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunologia. Rio de Janeiro, RJ. Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunologia. Rio de Janeiro, RJ. Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunologia. Rio de Janeiro, RJ. Brasil.L-arginine is involved in the production of both nitric oxide (NO), mediated by nitric oxide synthase (NOS) and L-ornithine, by arginase activity. It is generally accepted that NO regulation occurs mainly at the transcriptional level of NOS. In a previous work we purported that there is evidence that Leishmania sp. can produce NO from L-arginine. An arginase activity in its gene sequence has also been reported in Leishmania parasites. In a search for intracellular targets as potential antileishmanicidal agents, such as the L-arginine metabolism, we used 1,3,4-thiadiazolium mesoionic compounds, that have been demonstrated to be cytotoxic to the Leishmania amazonensis, when compared to Pentamidine isethionate as a reference drug. Parasites were assayed in absence/presence of 4'- and 3'-methoxy mesoionic derivatives in order to verify the effect on NO production and arginase activity in L. amazonensis. The results indicated that the drugs reduce from 70 to 90% of the NO production by the parasite and act on a soluble nitric oxide synthase purified from L. amazonensis promastigotes and axenic amastigotes.info:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZORIGINALLeonorL_Leon_etal_IOC_2008.pdfLeonorL_Leon_etal_IOC_2008.pdfapplication/pdf442059https://www.arca.fiocruz.br/bitstream/icict/32444/2/LeonorL_Leon_etal_IOC_2008.pdf3a58dab3266d52431ed8e7c5b3d66307MD52LICENSElicense.txtlicense.txttext/plain; charset=utf-82991https://www.arca.fiocruz.br/bitstream/icict/32444/3/license.txt5a560609d32a3863062d77ff32785d58MD53TEXTLeonorL_Leon_etal_IOC_2008.pdf.txtLeonorL_Leon_etal_IOC_2008.pdf.txtExtracted texttext/plain27651https://www.arca.fiocruz.br/bitstream/icict/32444/4/LeonorL_Leon_etal_IOC_2008.pdf.txt30b3f46668dba9c880391133b9545983MD54icict/324442019-04-13 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dc.title.pt_BR.fl_str_mv Effect of mesoionic 4-phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2-phenylamine chloride derivative salts on the activities of the nitric oxide synthase and arginase of Leishmania amazonensis
title Effect of mesoionic 4-phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2-phenylamine chloride derivative salts on the activities of the nitric oxide synthase and arginase of Leishmania amazonensis
spellingShingle Effect of mesoionic 4-phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2-phenylamine chloride derivative salts on the activities of the nitric oxide synthase and arginase of Leishmania amazonensis
Bezerra, Rômulo José Soares
Leishmania amazonensis
Óxido Nítrico
Leishmania amazonensis
Mesionic compounds
Phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2-phenylamine
Nitric oxide
Nitric oxide synthase
Arginase
Óxido Nítrico Sintase
Arginase
title_short Effect of mesoionic 4-phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2-phenylamine chloride derivative salts on the activities of the nitric oxide synthase and arginase of Leishmania amazonensis
title_full Effect of mesoionic 4-phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2-phenylamine chloride derivative salts on the activities of the nitric oxide synthase and arginase of Leishmania amazonensis
title_fullStr Effect of mesoionic 4-phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2-phenylamine chloride derivative salts on the activities of the nitric oxide synthase and arginase of Leishmania amazonensis
title_full_unstemmed Effect of mesoionic 4-phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2-phenylamine chloride derivative salts on the activities of the nitric oxide synthase and arginase of Leishmania amazonensis
title_sort Effect of mesoionic 4-phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2-phenylamine chloride derivative salts on the activities of the nitric oxide synthase and arginase of Leishmania amazonensis
author Bezerra, Rômulo José Soares
author_facet Bezerra, Rômulo José Soares
Silva, Edson F. da
Echevarria, Aurea
Silva, Liliane Gomes da
Finkelstein, Léa Cysne
Monteiro, Fabiane Pereira
Leon, Leonor L.
Genestra, Marcelo
author_role author
author2 Silva, Edson F. da
Echevarria, Aurea
Silva, Liliane Gomes da
Finkelstein, Léa Cysne
Monteiro, Fabiane Pereira
Leon, Leonor L.
Genestra, Marcelo
author2_role author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Bezerra, Rômulo José Soares
Silva, Edson F. da
Echevarria, Aurea
Silva, Liliane Gomes da
Finkelstein, Léa Cysne
Monteiro, Fabiane Pereira
Leon, Leonor L.
Genestra, Marcelo
dc.subject.other.pt_BR.fl_str_mv Leishmania amazonensis
Óxido Nítrico
topic Leishmania amazonensis
Óxido Nítrico
Leishmania amazonensis
Mesionic compounds
Phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2-phenylamine
Nitric oxide
Nitric oxide synthase
Arginase
Óxido Nítrico Sintase
Arginase
dc.subject.en.pt_BR.fl_str_mv Leishmania amazonensis
Mesionic compounds
Phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2-phenylamine
Nitric oxide
Nitric oxide synthase
Arginase
dc.subject.decs.pt_BR.fl_str_mv Óxido Nítrico Sintase
Arginase
description Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunologia. Rio de Janeiro, RJ. Brasil.
publishDate 2008
dc.date.issued.fl_str_mv 2008
dc.date.accessioned.fl_str_mv 2019-04-11T10:45:58Z
dc.date.available.fl_str_mv 2019-04-11T10:45:58Z
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.citation.fl_str_mv BEZERRA, Rômulo José Soares et al. Effect of mesoionic 4-phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2- phenylamine chloride derivative salts on the activities of the nitric oxide synthase and arginase of Leishmania amazonensis. Journal of Enzyme Inhibition and Medicinal Chemistry, v. 23, n. 3, p. 328–333, June 2008.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/32444
dc.identifier.issn.pt_BR.fl_str_mv 1475-6366
dc.identifier.doi.none.fl_str_mv 10.1080/14756360701585619
dc.identifier.eissn.none.fl_str_mv 1475-6374
identifier_str_mv BEZERRA, Rômulo José Soares et al. Effect of mesoionic 4-phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2- phenylamine chloride derivative salts on the activities of the nitric oxide synthase and arginase of Leishmania amazonensis. Journal of Enzyme Inhibition and Medicinal Chemistry, v. 23, n. 3, p. 328–333, June 2008.
1475-6366
10.1080/14756360701585619
1475-6374
url https://www.arca.fiocruz.br/handle/icict/32444
dc.language.iso.fl_str_mv eng
language eng
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dc.publisher.none.fl_str_mv Taylor & Francis
publisher.none.fl_str_mv Taylor & Francis
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instacron_str FIOCRUZ
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