Synthesis, Cruzain docking, and in vitro studies of aryl-4-oxothiazolylhydrazones against Trypanosoma cruzi.

Detalhes bibliográficos
Autor(a) principal: Leite, Ana Cristina Lima
Data de Publicação: 2007
Outros Autores: Lima, Renata Souza de, Moreira, Diogo Rodrigo Magalhães, Cardoso, Marcos Veríssimo de Oliveira, Brito, Ana Carolina Gouveia de, Santos, Luciene Maria Farias dos, Hernandes, Marcelo Zaldini, Kiperstok, Alice Costa, Lima, Ricardo Santana de, Soares, Milena Botelho Pereira
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/10036
Resumo: Universidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Laboratório de Planejamento. Avaliação e Síntese de Fármacos. Recife, PE, Brasil
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spelling Leite, Ana Cristina LimaLima, Renata Souza deMoreira, Diogo Rodrigo MagalhãesCardoso, Marcos Veríssimo de OliveiraBrito, Ana Carolina Gouveia deSantos, Luciene Maria Farias dosHernandes, Marcelo ZaldiniKiperstok, Alice CostaLima, Ricardo Santana deSoares, Milena Botelho Pereira2015-04-16T18:10:59Z2015-04-16T18:10:59Z2007LEITE, A. C. L. et al. Synthesis, cruzain docking, and in vitro studies of aryl-4-oxothiazolylhydrazones against Trypanosoma cruzi. Bioorganic & Medicinal Chemistry, v. 14, p. 3749–3757, 2007.1860-7187https://www.arca.fiocruz.br/handle/icict/1003610.1016/j.bmc.2006.01.034engElsevierSynthesis, Cruzain docking, and in vitro studies of aryl-4-oxothiazolylhydrazones against Trypanosoma cruzi.info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleUniversidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Laboratório de Planejamento. Avaliação e Síntese de Fármacos. Recife, PE, BrasilUniversidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Laboratório de Planejamento. Avaliação e Síntese de Fármacos. Recife, PE, BrasilUniversidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Laboratório de Planejamento. Avaliação e Síntese de Fármacos. Recife, PE, BrasilUniversidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Laboratório de Planejamento. Avaliação e Síntese de Fármacos. Recife, PE, BrasilUniversidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Laboratório de Planejamento. Avaliação e Síntese de Fármacos. Recife, PE, BrasilUniversidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Laboratório de Planejamento. Avaliação e Síntese de Fármacos. Recife, PE, BrasilUniversidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Laboratório de Química Teórica Medicinal. Recife, PE, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, BrasilResearch in recent years has demonstrated that the Trypanosoma cruzi cysteine protease cruzain (TCC) is a valid chemotherapeutic target. Herein we describe a small library of aryl-4-oxothiazolylhydrazones that have been tested in assays against T. cruzi cell cultures. The docking studies carried out suggest that these compounds are potential ligands for the TCC enzyme. The most promising compound of this series, N-(4-oxo-5-ethyl-2'-thiazolin-2-yl)-N'-phenylthio-(Z)-ethylidenehydrazone (6 f), was shown to be very active at non-cytotoxic concentrations in in vitro assays with mammalian cells and has a potency comparable with reference drugs such as nifurtimox (Nfx) and benznidazole (Bdz).Cisteína Endopeptidases/metabolismoHidrazonas/síntese químicaHidrazonas/farmacologiaProteínas de Protozoários/metabolismoTripanossomicidas/síntese químicaTripanossomicidas/farmacologiaTrypanosoma cruzi/efeitos de drogasAnimaisTécnicas In VitroEspectroscopia de Ressonância MagnéticaModelos Molecularesinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-82352https://www.arca.fiocruz.br/bitstream/icict/10036/1/license.txtafbdf7d7a9bcf771a1cc7edf5f618413MD51ORIGINALLeite A C L Synthesis, docking....pdfLeite A C L Synthesis, docking....pdfapplication/pdf610757https://www.arca.fiocruz.br/bitstream/icict/10036/2/Leite%20A%20C%20L%20Synthesis%2c%20docking....pdf9534d4781408434b33184616f3a5f517MD52TEXTLeite A C L Synthesis, docking....pdf.txtLeite A C L Synthesis, docking....pdf.txtExtracted texttext/plain34247https://www.arca.fiocruz.br/bitstream/icict/10036/3/Leite%20A%20C%20L%20Synthesis%2c%20docking....pdf.txtc293e31346b45bb79dbc6cd275a2f187MD53icict/100362023-03-15 14:33:06.77oai:www.arca.fiocruz.br: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ório InstitucionalPUBhttps://www.arca.fiocruz.br/oai/requestrepositorio.arca@fiocruz.bropendoar:21352023-03-15T17:33:06Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)false
dc.title.pt_BR.fl_str_mv Synthesis, Cruzain docking, and in vitro studies of aryl-4-oxothiazolylhydrazones against Trypanosoma cruzi.
title Synthesis, Cruzain docking, and in vitro studies of aryl-4-oxothiazolylhydrazones against Trypanosoma cruzi.
spellingShingle Synthesis, Cruzain docking, and in vitro studies of aryl-4-oxothiazolylhydrazones against Trypanosoma cruzi.
Leite, Ana Cristina Lima
Cisteína Endopeptidases/metabolismo
Hidrazonas/síntese química
Hidrazonas/farmacologia
Proteínas de Protozoários/metabolismo
Tripanossomicidas/síntese química
Tripanossomicidas/farmacologia
Trypanosoma cruzi/efeitos de drogas
Animais
Técnicas In Vitro
Espectroscopia de Ressonância Magnética
Modelos Moleculares
title_short Synthesis, Cruzain docking, and in vitro studies of aryl-4-oxothiazolylhydrazones against Trypanosoma cruzi.
title_full Synthesis, Cruzain docking, and in vitro studies of aryl-4-oxothiazolylhydrazones against Trypanosoma cruzi.
title_fullStr Synthesis, Cruzain docking, and in vitro studies of aryl-4-oxothiazolylhydrazones against Trypanosoma cruzi.
title_full_unstemmed Synthesis, Cruzain docking, and in vitro studies of aryl-4-oxothiazolylhydrazones against Trypanosoma cruzi.
title_sort Synthesis, Cruzain docking, and in vitro studies of aryl-4-oxothiazolylhydrazones against Trypanosoma cruzi.
author Leite, Ana Cristina Lima
author_facet Leite, Ana Cristina Lima
Lima, Renata Souza de
Moreira, Diogo Rodrigo Magalhães
Cardoso, Marcos Veríssimo de Oliveira
Brito, Ana Carolina Gouveia de
Santos, Luciene Maria Farias dos
Hernandes, Marcelo Zaldini
Kiperstok, Alice Costa
Lima, Ricardo Santana de
Soares, Milena Botelho Pereira
author_role author
author2 Lima, Renata Souza de
Moreira, Diogo Rodrigo Magalhães
Cardoso, Marcos Veríssimo de Oliveira
Brito, Ana Carolina Gouveia de
Santos, Luciene Maria Farias dos
Hernandes, Marcelo Zaldini
Kiperstok, Alice Costa
Lima, Ricardo Santana de
Soares, Milena Botelho Pereira
author2_role author
author
author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Leite, Ana Cristina Lima
Lima, Renata Souza de
Moreira, Diogo Rodrigo Magalhães
Cardoso, Marcos Veríssimo de Oliveira
Brito, Ana Carolina Gouveia de
Santos, Luciene Maria Farias dos
Hernandes, Marcelo Zaldini
Kiperstok, Alice Costa
Lima, Ricardo Santana de
Soares, Milena Botelho Pereira
dc.subject.decs.pt_BR.fl_str_mv Cisteína Endopeptidases/metabolismo
Hidrazonas/síntese química
Hidrazonas/farmacologia
Proteínas de Protozoários/metabolismo
Tripanossomicidas/síntese química
Tripanossomicidas/farmacologia
Trypanosoma cruzi/efeitos de drogas
Animais
Técnicas In Vitro
Espectroscopia de Ressonância Magnética
Modelos Moleculares
topic Cisteína Endopeptidases/metabolismo
Hidrazonas/síntese química
Hidrazonas/farmacologia
Proteínas de Protozoários/metabolismo
Tripanossomicidas/síntese química
Tripanossomicidas/farmacologia
Trypanosoma cruzi/efeitos de drogas
Animais
Técnicas In Vitro
Espectroscopia de Ressonância Magnética
Modelos Moleculares
description Universidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Laboratório de Planejamento. Avaliação e Síntese de Fármacos. Recife, PE, Brasil
publishDate 2007
dc.date.issued.fl_str_mv 2007
dc.date.accessioned.fl_str_mv 2015-04-16T18:10:59Z
dc.date.available.fl_str_mv 2015-04-16T18:10:59Z
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 LEITE, A. C. L. et al. Synthesis, cruzain docking, and in vitro studies of aryl-4-oxothiazolylhydrazones against Trypanosoma cruzi. Bioorganic & Medicinal Chemistry, v. 14, p. 3749–3757, 2007.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/10036
dc.identifier.issn.none.fl_str_mv 1860-7187
dc.identifier.doi.none.fl_str_mv 10.1016/j.bmc.2006.01.034
identifier_str_mv LEITE, A. C. L. et al. Synthesis, cruzain docking, and in vitro studies of aryl-4-oxothiazolylhydrazones against Trypanosoma cruzi. Bioorganic & Medicinal Chemistry, v. 14, p. 3749–3757, 2007.
1860-7187
10.1016/j.bmc.2006.01.034
url https://www.arca.fiocruz.br/handle/icict/10036
dc.language.iso.fl_str_mv eng
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dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
dc.source.none.fl_str_mv reponame:Repositório Institucional da FIOCRUZ (ARCA)
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