Mechanism of action of a Nitroimidazole-Thiadiazole derivate upon Trypanosoma cruzi tissue culture amastigotes

Detalhes bibliográficos
Autor(a) principal: Castro, Solange L. de
Data de Publicação: 1990
Outros Autores: Meirelles, Maria de Nazareth L. de
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/43360
Resumo: Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Ultraestrutura e Biologia Celular. Rio de Janeiro, RJ, Brasil.
id CRUZ_bee83d3cf890dc1c52016a53ea6399f3
oai_identifier_str oai:www.arca.fiocruz.br:icict/43360
network_acronym_str CRUZ
network_name_str Repositório Institucional da FIOCRUZ (ARCA)
repository_id_str 2135
spelling Castro, Solange L. deMeirelles, Maria de Nazareth L. de2020-09-14T18:45:07Z2020-09-14T18:45:07Z1990CASTRO, Solange L. de; MEIRELLES, Maria de Nazareth L. Mechanism of action of a nitroimidazole-thiadiazole derivate upon Trypanosoma cruzi tissue culture amastigotes. Memórias do Instituto Oswaldo Cruz, Rio de Janeiro, v. 85, n. 1, p. 95-99, jan./mar. 1990.0074-0276https://www.arca.fiocruz.br/handle/icict/4336010.1590/S0074-027619900001000161678-8060engFundação Oswaldo Cruz. Instituto Oswaldo Cruz.Trypanosoma cruziAgentes quimioterápicosAmastigotasBiossíntese de macromoléculasPrecursores radioativosAção do derivado de tiadiazolMegazolTrypanosoma cruziChemoterapeutic agentsAmastigotesMacromolecule biosynthesisRadiactive precursorsAction of thiadiazole derivateMegazolMechanism of action of a Nitroimidazole-Thiadiazole derivate upon Trypanosoma cruzi tissue culture amastigotesinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Ultraestrutura e Biologia Celular. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Ultraestrutura e Biologia Celular. Rio de Janeiro, RJ, Brasil.Megazol (CL 64,855) a very effective drug in experimental infections by Trypanosoma cruzi, and also in in vitro assays with vertebrate forms of the parasite, had its parasite, had its activity upon macromolecule biosynthesis tested using tissue culture-derived amastigote forms. Megazol presented a drastic inhibition of [3H]-uridine incorporation, suggesting a selective activity upon protein synthesis. Comparing the three drugs, megazol was more potent than nifurtimox and benznidazole in inhibiting protein an DNA synthesis. Megazol showed a 91% of inhibition of [3H]-leucine incorporation whereas nifurtimox and benznidazole, 0% and 2%, respectively. These latter two drugs inhibited the incorporation of all the precursors tested at similar levels, but the concentration of benznidazole was always three times higher, suggesting different mechanisms of action or, more probably, a greater efficiency of the 5-nitrofuran derivate in relation to the 2-nitroimidazole. So, wes conclude that the mode of action of megazol is different from the ones of nifurtimox and benznidazole and that its primary effect is associated with an impairment of protein synthesis.info:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-82991https://www.arca.fiocruz.br/bitstream/icict/43360/1/license.txt5a560609d32a3863062d77ff32785d58MD51ORIGINALSolangeCastro_MariaNMeirelles_IOC_1990.pdfSolangeCastro_MariaNMeirelles_IOC_1990.pdfapplication/pdf247274https://www.arca.fiocruz.br/bitstream/icict/43360/2/SolangeCastro_MariaNMeirelles_IOC_1990.pdf7999874038689b385fe73cd15db3d031MD52TEXTSolangeCastro_MariaNMeirelles_IOC_1990.pdf.txtSolangeCastro_MariaNMeirelles_IOC_1990.pdf.txtExtracted texttext/plain5https://www.arca.fiocruz.br/bitstream/icict/43360/3/SolangeCastro_MariaNMeirelles_IOC_1990.pdf.txtcc9067c2ee470dc248b14b194209a34eMD53icict/433602020-09-15 02:04:49.448oai:www.arca.fiocruz.br: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ório InstitucionalPUBhttps://www.arca.fiocruz.br/oai/requestrepositorio.arca@fiocruz.bropendoar:21352020-09-15T05:04:49Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)false
dc.title.pt_BR.fl_str_mv Mechanism of action of a Nitroimidazole-Thiadiazole derivate upon Trypanosoma cruzi tissue culture amastigotes
title Mechanism of action of a Nitroimidazole-Thiadiazole derivate upon Trypanosoma cruzi tissue culture amastigotes
spellingShingle Mechanism of action of a Nitroimidazole-Thiadiazole derivate upon Trypanosoma cruzi tissue culture amastigotes
Castro, Solange L. de
Trypanosoma cruzi
Agentes quimioterápicos
Amastigotas
Biossíntese de macromoléculas
Precursores radioativos
Ação do derivado de tiadiazol
Megazol
Trypanosoma cruzi
Chemoterapeutic agents
Amastigotes
Macromolecule biosynthesis
Radiactive precursors
Action of thiadiazole derivate
Megazol
title_short Mechanism of action of a Nitroimidazole-Thiadiazole derivate upon Trypanosoma cruzi tissue culture amastigotes
title_full Mechanism of action of a Nitroimidazole-Thiadiazole derivate upon Trypanosoma cruzi tissue culture amastigotes
title_fullStr Mechanism of action of a Nitroimidazole-Thiadiazole derivate upon Trypanosoma cruzi tissue culture amastigotes
title_full_unstemmed Mechanism of action of a Nitroimidazole-Thiadiazole derivate upon Trypanosoma cruzi tissue culture amastigotes
title_sort Mechanism of action of a Nitroimidazole-Thiadiazole derivate upon Trypanosoma cruzi tissue culture amastigotes
author Castro, Solange L. de
author_facet Castro, Solange L. de
Meirelles, Maria de Nazareth L. de
author_role author
author2 Meirelles, Maria de Nazareth L. de
author2_role author
dc.contributor.author.fl_str_mv Castro, Solange L. de
Meirelles, Maria de Nazareth L. de
dc.subject.other.pt_BR.fl_str_mv Trypanosoma cruzi
Agentes quimioterápicos
Amastigotas
Biossíntese de macromoléculas
Precursores radioativos
Ação do derivado de tiadiazol
Megazol
topic Trypanosoma cruzi
Agentes quimioterápicos
Amastigotas
Biossíntese de macromoléculas
Precursores radioativos
Ação do derivado de tiadiazol
Megazol
Trypanosoma cruzi
Chemoterapeutic agents
Amastigotes
Macromolecule biosynthesis
Radiactive precursors
Action of thiadiazole derivate
Megazol
dc.subject.en.pt_BR.fl_str_mv Trypanosoma cruzi
Chemoterapeutic agents
Amastigotes
Macromolecule biosynthesis
Radiactive precursors
Action of thiadiazole derivate
Megazol
description Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Ultraestrutura e Biologia Celular. Rio de Janeiro, RJ, Brasil.
publishDate 1990
dc.date.issued.fl_str_mv 1990
dc.date.accessioned.fl_str_mv 2020-09-14T18:45:07Z
dc.date.available.fl_str_mv 2020-09-14T18:45:07Z
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 CASTRO, Solange L. de; MEIRELLES, Maria de Nazareth L. Mechanism of action of a nitroimidazole-thiadiazole derivate upon Trypanosoma cruzi tissue culture amastigotes. Memórias do Instituto Oswaldo Cruz, Rio de Janeiro, v. 85, n. 1, p. 95-99, jan./mar. 1990.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/43360
dc.identifier.issn.pt_BR.fl_str_mv 0074-0276
dc.identifier.doi.none.fl_str_mv 10.1590/S0074-02761990000100016
dc.identifier.eissn.none.fl_str_mv 1678-8060
identifier_str_mv CASTRO, Solange L. de; MEIRELLES, Maria de Nazareth L. Mechanism of action of a nitroimidazole-thiadiazole derivate upon Trypanosoma cruzi tissue culture amastigotes. Memórias do Instituto Oswaldo Cruz, Rio de Janeiro, v. 85, n. 1, p. 95-99, jan./mar. 1990.
0074-0276
10.1590/S0074-02761990000100016
1678-8060
url https://www.arca.fiocruz.br/handle/icict/43360
dc.language.iso.fl_str_mv eng
language eng
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv Fundação Oswaldo Cruz. Instituto Oswaldo Cruz.
publisher.none.fl_str_mv Fundação Oswaldo Cruz. Instituto Oswaldo Cruz.
dc.source.none.fl_str_mv reponame:Repositório Institucional da FIOCRUZ (ARCA)
instname:Fundação Oswaldo Cruz (FIOCRUZ)
instacron:FIOCRUZ
instname_str Fundação Oswaldo Cruz (FIOCRUZ)
instacron_str FIOCRUZ
institution FIOCRUZ
reponame_str Repositório Institucional da FIOCRUZ (ARCA)
collection Repositório Institucional da FIOCRUZ (ARCA)
bitstream.url.fl_str_mv https://www.arca.fiocruz.br/bitstream/icict/43360/1/license.txt
https://www.arca.fiocruz.br/bitstream/icict/43360/2/SolangeCastro_MariaNMeirelles_IOC_1990.pdf
https://www.arca.fiocruz.br/bitstream/icict/43360/3/SolangeCastro_MariaNMeirelles_IOC_1990.pdf.txt
bitstream.checksum.fl_str_mv 5a560609d32a3863062d77ff32785d58
7999874038689b385fe73cd15db3d031
cc9067c2ee470dc248b14b194209a34e
bitstream.checksumAlgorithm.fl_str_mv MD5
MD5
MD5
repository.name.fl_str_mv Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)
repository.mail.fl_str_mv repositorio.arca@fiocruz.br
_version_ 1813009202766938112

Registros relacionados