In Vitro, In Silico, and In Vivo Analyses of Novel Aromatic Amidines against Trypanosoma cruzi
| Autor(a) principal: | |
|---|---|
| Data de Publicação: | 2018 |
| 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/28840 |
Resumo: | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil. |
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Santos, Camila C.Lionel, Jéssica R.Peres, Raiza B.Batista, Marcos M.Silva, Patrícia B. daOliveira, Gabriel M. deSilva, Cristiane F. daBatista, Denise G. J.Souza, Sandra Maria O.Andrade, Carolina H.Neves, Bruno J.Braga, Rodolpho C.Patrick, Donald A.Bakunova, Svetlana M.Tidwell, Richard R.Soeiro, Maria de Nazaré C.2018-09-18T11:12:05Z2018-09-18T11:12:05Z2018SANTOS, Camila C. et al. In Vitro, In Silico, and In Vivo Analyses of Novel Aromatic Amidines against Trypanosoma cruzi. Antimicrobial Agents and Chemotherapy, v. 62, n. 2, p. 1-8, 2018.0066-4804https://www.arca.fiocruz.br/handle/icict/2884010.1128/AAC.02205-171098-6596engAmerican Society for MicrobiologyDoença de ChagasQuimioterapia experimentalIn vivoChagas diseasearylimidamidesexperimental chemotherapyin vivoIn Vitro, In Silico, and In Vivo Analyses of Novel Aromatic Amidines 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.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 Estrutural. Rio de Janeiro, RJ, Brasil.Universidade Federal de Goiás. Faculdade de Farmácia. Laboratório de Planejamento de Fármacos e Modelagem Molecular. Goiânia, GO, Brasil.Universidade Federal de Goiás. Faculdade de Farmácia. Laboratório de Planejamento de Fármacos e Modelagem Molecular. Goiânia, GO, Brasil.Universidade Federal de Goiás. Faculdade de Farmácia. Laboratório de Planejamento de Fármacos e Modelagem Molecular. Goiânia, GO, Brasil.University of North Carolina School of Medicine. Department of Pathology and Laboratory Medicine. Chapel Hill, North Carolina, USA.University of North Carolina School of Medicine. Department of Pathology and Laboratory Medicine. Chapel Hill, North Carolina, USA.University of North Carolina School of Medicine. 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.Five bis-arylimidamides were assayed as anti-Trypanosoma cruzi agents by in vitro, in silico, and in vivo approaches. None were considered to be pan-assay interference compounds. They had a favorable pharmacokinetic landscape and were active against trypomastigotes and intracellular forms, and in combination with benznidazole, they gave no interaction. The most selective agent (28SMB032) tested in vivo led to a 40% reduction in parasitemia (0.1 mg/kg of body weight/5 days intraperitoneally) but without mortality protection. In silico target fishing suggested DNA as the main target, but ultrastructural data did not match.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/28840/1/license.txt5a560609d32a3863062d77ff32785d58MD51ORIGINALcamilac_santos_etal_IOC_2018.pdfcamilac_santos_etal_IOC_2018.pdfapplication/pdf1510719https://www.arca.fiocruz.br/bitstream/icict/28840/2/camilac_santos_etal_IOC_2018.pdf13055b3e624dd59ee79e2da2fe4324ceMD52TEXTcamilac_santos_etal_IOC_2018.pdf.txtcamilac_santos_etal_IOC_2018.pdf.txtExtracted texttext/plain27622https://www.arca.fiocruz.br/bitstream/icict/28840/3/camilac_santos_etal_IOC_2018.pdf.txt177fe62adaf99a9cd88a9e092fc0cf30MD53icict/288402023-09-05 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| dc.title.pt_BR.fl_str_mv |
In Vitro, In Silico, and In Vivo Analyses of Novel Aromatic Amidines against Trypanosoma cruzi |
| title |
In Vitro, In Silico, and In Vivo Analyses of Novel Aromatic Amidines against Trypanosoma cruzi |
| spellingShingle |
In Vitro, In Silico, and In Vivo Analyses of Novel Aromatic Amidines against Trypanosoma cruzi Santos, Camila C. Doença de Chagas Quimioterapia experimental In vivo Chagas disease arylimidamides experimental chemotherapy in vivo |
| title_short |
In Vitro, In Silico, and In Vivo Analyses of Novel Aromatic Amidines against Trypanosoma cruzi |
| title_full |
In Vitro, In Silico, and In Vivo Analyses of Novel Aromatic Amidines against Trypanosoma cruzi |
| title_fullStr |
In Vitro, In Silico, and In Vivo Analyses of Novel Aromatic Amidines against Trypanosoma cruzi |
| title_full_unstemmed |
In Vitro, In Silico, and In Vivo Analyses of Novel Aromatic Amidines against Trypanosoma cruzi |
| title_sort |
In Vitro, In Silico, and In Vivo Analyses of Novel Aromatic Amidines against Trypanosoma cruzi |
| author |
Santos, Camila C. |
| author_facet |
Santos, Camila C. Lionel, Jéssica R. Peres, Raiza B. Batista, Marcos M. Silva, Patrícia B. da Oliveira, Gabriel M. de Silva, Cristiane F. da Batista, Denise G. J. Souza, Sandra Maria O. Andrade, Carolina H. Neves, Bruno J. Braga, Rodolpho C. Patrick, Donald A. Bakunova, Svetlana M. Tidwell, Richard R. Soeiro, Maria de Nazaré C. |
| author_role |
author |
| author2 |
Lionel, Jéssica R. Peres, Raiza B. Batista, Marcos M. Silva, Patrícia B. da Oliveira, Gabriel M. de Silva, Cristiane F. da Batista, Denise G. J. Souza, Sandra Maria O. Andrade, Carolina H. Neves, Bruno J. Braga, Rodolpho C. Patrick, Donald A. Bakunova, Svetlana M. Tidwell, Richard R. Soeiro, Maria de Nazaré C. |
| author2_role |
author author author author author author author author author author author author author author author |
| dc.contributor.author.fl_str_mv |
Santos, Camila C. Lionel, Jéssica R. Peres, Raiza B. Batista, Marcos M. Silva, Patrícia B. da Oliveira, Gabriel M. de Silva, Cristiane F. da Batista, Denise G. J. Souza, Sandra Maria O. Andrade, Carolina H. Neves, Bruno J. Braga, Rodolpho C. Patrick, Donald A. Bakunova, Svetlana M. Tidwell, Richard R. Soeiro, Maria de Nazaré C. |
| dc.subject.other.pt_BR.fl_str_mv |
Doença de Chagas Quimioterapia experimental In vivo |
| topic |
Doença de Chagas Quimioterapia experimental In vivo Chagas disease arylimidamides experimental chemotherapy in vivo |
| dc.subject.en.pt_BR.fl_str_mv |
Chagas disease arylimidamides experimental chemotherapy in vivo |
| description |
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil. |
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2018 |
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2018-09-18T11:12:05Z |
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2018-09-18T11:12:05Z |
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2018 |
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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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SANTOS, Camila C. et al. In Vitro, In Silico, and In Vivo Analyses of Novel Aromatic Amidines against Trypanosoma cruzi. Antimicrobial Agents and Chemotherapy, v. 62, n. 2, p. 1-8, 2018. |
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https://www.arca.fiocruz.br/handle/icict/28840 |
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0066-4804 |
| dc.identifier.doi.none.fl_str_mv |
10.1128/AAC.02205-17 |
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1098-6596 |
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SANTOS, Camila C. et al. In Vitro, In Silico, and In Vivo Analyses of Novel Aromatic Amidines against Trypanosoma cruzi. Antimicrobial Agents and Chemotherapy, v. 62, n. 2, p. 1-8, 2018. 0066-4804 10.1128/AAC.02205-17 1098-6596 |
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eng |
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eng |
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American Society for Microbiology |
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American Society for Microbiology |
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