In Vitro and In Vivo Biological Effects of Novel Arylimidamide Derivatives against Trypanosoma cruzi

Detalhes bibliográficos
Autor(a) principal: Timm, Bruno Lisboa
Data de Publicação: 2014
Outros Autores: Silva, Patrícia Bernardino da, Batista, Marcos Meuser, Silva, Francisca Hildemagna Guedes da, Silva, Cristiane França da, Todwell, Richard R., Patrick, Donald A., Jones, Susan Kilgore, Bakunov, Stanislav A., Bakunova, Svetlana M., Soeiro, Maria de Nazaré C.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/10056
Resumo: Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.
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spelling Timm, Bruno LisboaSilva, Patrícia Bernardino daBatista, Marcos MeuserSilva, Francisca Hildemagna Guedes daSilva, Cristiane França daTodwell, Richard R.Patrick, Donald A.Jones, Susan KilgoreBakunov, Stanislav A.Bakunova, Svetlana M.Soeiro, Maria de Nazaré C.2015-04-17T17:04:28Z2015-04-17T17:04:28Z2014TIMM, Bruno Lisboa et al. In Vitro and In Vivo Biological Effects of Novel Arylimidamide Derivatives against Trypanosoma cruzi. Antimicrobial Agents and Chemotherapy, v. 58, n.7, p. 3720-3726, Jul. 2014.https://www.arca.fiocruz.br/handle/icict/1005610.1128/AAC.02353-14engAmerican Society for MicrobiologyDoença de ChagasTripanosoma CruziQuimioterapiaIn vitroChagas DiseaseTripanosoma CruziChemotherapyIn vitroIn vitroCaracterísticas dos EstudosIn Vitro and In Vivo Biological Effects of Novel Arylimidamide Derivatives against Trypanosoma cruziinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.University of North Carolina. Department of Pathology and Laboratory Medicine. Chapel Hill, North Carolina, USA.University of North Carolina. Department of Pathology and Laboratory Medicine. Chapel Hill, North Carolina, USA.University of North Carolina. Department of Pathology and Laboratory Medicine. Chapel Hill, North Carolina, USA.University of North Carolina. Department of Pathology and Laboratory Medicine. Chapel Hill, North Carolina, USA.University of North Carolina. Department of Pathology and Laboratory Medicine. Chapel Hill, North Carolina, USA.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.Chagas disease (CD), a neglected tropical disease caused by Trypanosoma cruzi, remains a serious public health problem in several Latin American countries. The available chemotherapies for CD have limited efficacy and exhibit undesirable side effects. Aromatic diamidines and arylimidamides (AIAs) have shown broad-spectrum activity against intracellular parasites, including T. cruzi. Therefore, our aim was to evaluate the biological activity of eight novel AIAs (16DAP002, 16SAB079, 18SAB075, 23SMB022, 23SMB026, 23SMB054, 26SMB070, and 27SMB009) against experimental models of T. cruzi infection in vitro and in vivo. Our data show that none of the compounds induced a loss of cellular viability up to 32 M. Two AIAs, 18SAB075 and 16DAP002, exhibited good in vitro activity against different parasite strains (Y and Tulahuen) and against the two relevant forms of the parasite for mammalian hosts. Due to the excellent selective indexes of 18SAB075, this AIA was moved to in vivo tests for acute toxicity and parasite efficacy; nontoxic doses (no-observed-adverse-effect level [NOAEL], 50 mg/kg) were employed in the tests for parasite efficacy. In experimental models of acute T. cruzi infection, 18SAB075 reduced parasitemia levels only up to 50% and led to 40% protection against mortality (at 5 mg/kg of body weight), being less effective than the reference drug, benznidazole.info:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txttext/plain1914https://www.arca.fiocruz.br/bitstream/icict/10056/1/license.txt7d48279ffeed55da8dfe2f8e81f3b81fMD51ORIGINALbruno_timmetal_IOC_2014.pdfapplication/pdf984025https://www.arca.fiocruz.br/bitstream/icict/10056/2/bruno_timmetal_IOC_2014.pdf9793d51f701f7a0d19ee59f53199681aMD52TEXTbruno_timmetal_IOC_2014.pdf.txtbruno_timmetal_IOC_2014.pdf.txtExtracted texttext/plain33745https://www.arca.fiocruz.br/bitstream/icict/10056/3/bruno_timmetal_IOC_2014.pdf.txtebf5bb6d2cdeef5d927971317b0d79ccMD53icict/100562022-06-24 13:11:06.122oai:www.arca.fiocruz.br:icict/10056TElDRU7Dh0EgREUgRElTVFJJQlVJw4fDg08gTsODTy1FWENMVVNJVkEKCkFvIGNvbmNvcmRhciBlIGFjZWl0YXIgZXN0YSBsaWNlbsOnYSB2b2PDqiAoYXV0b3Igb3UgZGV0ZW50b3IgZG9zIGRpcmVpdG9zIGF1dG9yYWlzKToKCmEpIERlY2xhcmEgcXVlIGNvbmhlY2UgYSBwb2zDrXRpY2EgZGUgY29weXJpZ2h0IGRhIGVkaXRvcmEgZG8gc2V1IGRvY3VtZW50by4KCmIpIERlY2xhcmEgcXVlIGNvbmhlY2UgZSBhY2VpdGEgYXMgRGlyZXRyaXplcyBwYXJhIG8gUmVwb3NpdMOzcmlvIEluc3RpdHVjaW9uYWwgZGEgRnVuZGHDp8OjbyBPc3dhbGRvIENydXogKEZJT0NSVVopLgoKYykgQ29uY2VkZSDDoCBGSU9DUlVaIG8gZGlyZWl0byBuw6NvLWV4Y2x1c2l2byBkZSBhcnF1aXZhciwgcmVwcm9kdXppciwgY29udmVydGVyIChjb21vIGRlZmluaWRvIGEgc2VndWlyKSwgY29tdW5pY2FyCiAKZS9vdSBkaXN0cmlidWlyIG5vIFJlcG9zaXTDs3JpbyBkYSBGSU9DUlVaLCBvIGRvY3VtZW50byBlbnRyZWd1ZSAoaW5jbHVpbmRvIG8gcmVzdW1vL2Fic3RyYWN0KSBlbSBmb3JtYXRvIGRpZ2l0YWwgb3UgCgpwb3IgcXVhbHF1ZXIgb3V0cm8gbWVpby4KCmQpIERlY2xhcmEgcXVlIGF1dG9yaXphIGEgRklPQ1JVWiBhIGFycXVpdmFyIG1haXMgZGUgdW1hIGPDs3BpYSBkZXN0ZSBkb2N1bWVudG8gZSBjb252ZXJ0w6otbG8sIHNlbSBhbHRlcmFyIG8gc2V1IGNvbnRlw7pkbywgCgpwYXJhIHF1YWxxdWVyIGZvcm1hdG8gZGUgYXJxdWl2bywgbWVpbyBvdSBzdXBvcnRlLCBwYXJhIGVmZWl0b3MgZGUgc2VndXJhbsOnYSwgcHJlc2VydmHDp8OjbyAoYmFja3VwKSBlIGFjZXNzby4KCmUpIERlY2xhcmEgcXVlIG8gZG9jdW1lbnRvIHN1Ym1ldGlkbyDDqSBvIHNldSB0cmFiYWxobyBvcmlnaW5hbCwgZSBxdWUgZGV0w6ltIG8gZGlyZWl0byBkZSBjb25jZWRlciBhIHRlcmNlaXJvcyBvcyBkaXJlaXRvcyAKCmNvbnRpZG9zIG5lc3RhIGxpY2Vuw6dhLiBEZWNsYXJhIHRhbWLDqW0gcXVlIGEgZW50cmVnYSBkbyBkb2N1bWVudG8gbsOjbyBpbmZyaW5nZSBvcyBkaXJlaXRvcyBkZSBxdWFscXVlciBvdXRyYSBwZXNzb2Egb3UgZW50aWRhZGUuCgpmKSBEZWNsYXJhIHF1ZSwgbm8gY2FzbyBkbyBkb2N1bWVudG8gc3VibWV0aWRvIGNvbnRlciBtYXRlcmlhbCBkbyBxdWFsIG7Do28gZGV0w6ltIG9zIGRpcmVpdG9zIGRlIGF1dG9yLCBvYnRldmUgYSBhdXRvcml6YcOnw6NvIAoKaXJyZXN0cml0YSBkbyByZXNwZWN0aXZvIGRldGVudG9yIGRlc3NlcyBkaXJlaXRvcywgcGFyYSBjZWRlciBhIEZJT0NSVVogb3MgZGlyZWl0b3MgcmVxdWVyaWRvcyBwb3IgZXN0YSBMaWNlbsOnYSBlIGF1dG9yaXphciBhIAoKdXRpbGl6w6EtbG9zIGxlZ2FsbWVudGUuIERlY2xhcmEgdGFtYsOpbSBxdWUgZXNzZSBtYXRlcmlhbCBjdWpvcyBkaXJlaXRvcyBzw6NvIGRlIHRlcmNlaXJvcyBlc3TDoSBjbGFyYW1lbnRlIGlkZW50aWZpY2FkbyBlIHJlY29uaGVjaWRvIAoKbm8gdGV4dG8gb3UgY29udGXDumRvIGRvIGRvY3VtZW50byBlbnRyZWd1ZS4KCmcpIFNFIE8gRE9DVU1FTlRPIEVOVFJFR1VFIMOJIEJBU0VBRE8gRU0gVFJBQkFMSE8gRklOQU5DSUFETyBPVSBBUE9JQURPIFBPUiBPVVRSQSBJTlNUSVRVScOHw4NPIFFVRSBOw4NPIEEgRklPQ1JVWiwgREVDTEFSQSBRVUUgQ1VNUFJJVSAKClFVQUlTUVVFUiBPQlJJR0HDh8OVRVMgRVhJR0lEQVMgUEVMTyBSRVNQRUNUSVZPIENPTlRSQVRPIE9VIEFDT1JETy4gQSBGSU9DUlVaIGlkZW50aWZpY2Fyw6EgY2xhcmFtZW50ZSBvKHMpIG5vbWUocykgZG8ocykgYXV0b3IoZXMpIGRvcyAKCmRpcmVpdG9zIGRvIGRvY3VtZW50byBlbnRyZWd1ZSBlIG7Do28gZmFyw6EgcXVhbHF1ZXIgYWx0ZXJhw6fDo28sIHBhcmEgYWzDqW0gZG8gcHJldmlzdG8gbmEgYWzDrW5lYSBjKS4KRepositório InstitucionalPUBhttps://www.arca.fiocruz.br/oai/requestrepositorio.arca@fiocruz.bropendoar:21352022-06-24T16:11:06Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)false
dc.title.pt_BR.fl_str_mv In Vitro and In Vivo Biological Effects of Novel Arylimidamide Derivatives against Trypanosoma cruzi
title In Vitro and In Vivo Biological Effects of Novel Arylimidamide Derivatives against Trypanosoma cruzi
spellingShingle In Vitro and In Vivo Biological Effects of Novel Arylimidamide Derivatives against Trypanosoma cruzi
Timm, Bruno Lisboa
Doença de Chagas
Tripanosoma Cruzi
Quimioterapia
In vitro
Chagas Disease
Tripanosoma Cruzi
Chemotherapy
In vitro
In vitro
Características dos Estudos
title_short In Vitro and In Vivo Biological Effects of Novel Arylimidamide Derivatives against Trypanosoma cruzi
title_full In Vitro and In Vivo Biological Effects of Novel Arylimidamide Derivatives against Trypanosoma cruzi
title_fullStr In Vitro and In Vivo Biological Effects of Novel Arylimidamide Derivatives against Trypanosoma cruzi
title_full_unstemmed In Vitro and In Vivo Biological Effects of Novel Arylimidamide Derivatives against Trypanosoma cruzi
title_sort In Vitro and In Vivo Biological Effects of Novel Arylimidamide Derivatives against Trypanosoma cruzi
author Timm, Bruno Lisboa
author_facet Timm, Bruno Lisboa
Silva, Patrícia Bernardino da
Batista, Marcos Meuser
Silva, Francisca Hildemagna Guedes da
Silva, Cristiane França da
Todwell, Richard R.
Patrick, Donald A.
Jones, Susan Kilgore
Bakunov, Stanislav A.
Bakunova, Svetlana M.
Soeiro, Maria de Nazaré C.
author_role author
author2 Silva, Patrícia Bernardino da
Batista, Marcos Meuser
Silva, Francisca Hildemagna Guedes da
Silva, Cristiane França da
Todwell, Richard R.
Patrick, Donald A.
Jones, Susan Kilgore
Bakunov, Stanislav A.
Bakunova, Svetlana M.
Soeiro, Maria de Nazaré C.
author2_role author
author
author
author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Timm, Bruno Lisboa
Silva, Patrícia Bernardino da
Batista, Marcos Meuser
Silva, Francisca Hildemagna Guedes da
Silva, Cristiane França da
Todwell, Richard R.
Patrick, Donald A.
Jones, Susan Kilgore
Bakunov, Stanislav A.
Bakunova, Svetlana M.
Soeiro, Maria de Nazaré C.
dc.subject.other.pt_BR.fl_str_mv Doença de Chagas
Tripanosoma Cruzi
Quimioterapia
In vitro
topic Doença de Chagas
Tripanosoma Cruzi
Quimioterapia
In vitro
Chagas Disease
Tripanosoma Cruzi
Chemotherapy
In vitro
In vitro
Características dos Estudos
dc.subject.en.pt_BR.fl_str_mv Chagas Disease
Tripanosoma Cruzi
Chemotherapy
In vitro
dc.subject.decs.pt_BR.fl_str_mv In vitro
Características dos Estudos
description Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.
publishDate 2014
dc.date.issued.fl_str_mv 2014
dc.date.accessioned.fl_str_mv 2015-04-17T17:04:28Z
dc.date.available.fl_str_mv 2015-04-17T17:04:28Z
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 TIMM, Bruno Lisboa et al. In Vitro and In Vivo Biological Effects of Novel Arylimidamide Derivatives against Trypanosoma cruzi. Antimicrobial Agents and Chemotherapy, v. 58, n.7, p. 3720-3726, Jul. 2014.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/10056
dc.identifier.doi.pt_BR.fl_str_mv 10.1128/AAC.02353-14
identifier_str_mv TIMM, Bruno Lisboa et al. In Vitro and In Vivo Biological Effects of Novel Arylimidamide Derivatives against Trypanosoma cruzi. Antimicrobial Agents and Chemotherapy, v. 58, n.7, p. 3720-3726, Jul. 2014.
10.1128/AAC.02353-14
url https://www.arca.fiocruz.br/handle/icict/10056
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 American Society for Microbiology
publisher.none.fl_str_mv American Society for Microbiology
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
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reponame_str Repositório Institucional da FIOCRUZ (ARCA)
collection Repositório Institucional da FIOCRUZ (ARCA)
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