In Vitro and In Vivo Biological Effects of Novel Arylimidamide Derivatives against Trypanosoma cruzi
| Autor(a) principal: | |
|---|---|
| Data de Publicação: | 2014 |
| Outros Autores: | , , , , , , , , , |
| 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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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: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ório 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 |
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Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil. |
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2014 |
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2014 |
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2015-04-17T17:04:28Z |
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2015-04-17T17:04:28Z |
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info:eu-repo/semantics/publishedVersion |
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info:eu-repo/semantics/article |
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article |
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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. |
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https://www.arca.fiocruz.br/handle/icict/10056 |
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10.1128/AAC.02353-14 |
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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 |
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American Society for Microbiology |
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American Society for Microbiology |
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