Exploring the potential activity spectrum of two 5-nitroindazolinone prototypes on different Trypanosoma cruzi strains
| Autor(a) principal: | |
|---|---|
| Data de Publicação: | 2015 |
| 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/13247 |
Resumo: | UCM-UPM & CSIC. CEI Campus Moncloa. Madrid, Spain / Universidad Complutense de Madrid. Facultad de Farmacia. Departamento de Parasitologia. Madrid, Spain. |
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Fonseca-Berzal, CristinaSilva, Patricia Bernardino daSilva, Cristiane FrançaVasconcelos, MarianeBatista, Marcos MeuserEscario, José A.Arán, Vicente J.Gómez-Barrio, AliciaSoeiro, Maria de Nazaré C.2016-03-22T17:27:09Z2016-03-22T17:27:09Z2015FONSECA-BERZAL, Cristina; et al. Exploring the potential activity spectrum of two 5-nitroindazolinone prototypes on different Trypanosoma cruzi strains. Parasitology Open, v.1, e1, 10p, 2015.https://www.arca.fiocruz.br/handle/icict/13247:10.1017/pao.2015.42055-7094engCambridge University PressExploring the potential activity spectrum of two 5-nitroindazolinone prototypes on different Trypanosoma cruzi strainsinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleUCM-UPM & CSIC. CEI Campus Moncloa. Madrid, Spain / Universidad Complutense de Madrid. Facultad de Farmacia. Departamento de Parasitologia. Madrid, Spain.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.UCM-UPM & CSIC. CEI Campus Moncloa. Madrid, Spain / Universidad Complutense de Madrid. Facultad de Farmacia. Departamento de Parasitologia. Madrid, Spain.UCM-UPM & CSIC. CEI Campus Moncloa. Madrid, Spain / Consejo Superior de Investigaciones Científicas (CSIC). Instituto de Química Médica (IQM),. Madrid, Spain.UCM-UPM & CSIC. CEI Campus Moncloa. Madrid, Spain / Universidad Complutense de Madrid. Facultad de Farmacia. Departamento de Parasitologia. Madrid, Spain.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil.In the present study, the potential activity of two 5-nitroindazole derivatives previously proposed as suitable antichagasic prototypes was further evaluated on diverse Trypanosoma cruzistrains belonging to two discrete typing units (DTUs) frequently associated with human infection (i.e. DTUs TcII and TcVI). The trypanocidal profile that both 2-benzyl-1-propyl (22) and 2-benzyl-1-butyl (24) derivatives achieved on Tulahuen amastigotes (IC50 = 3·56 ± 0·99 and 6·31 ± 1·04 µM, respectively) correlates with that of formerly obtained on CL Brener, corroborating an outstanding activity on DTU TcVI parasites. Moreover, a sequential screening on extracellular and intracellular stages of T. cruzi Y (DTU TcII) demonstrated also the effectiveness of 22 and 24 over this strain on a similar range of activity (IC50 epimastigotes = 3·55 ± 0·47 and 7·92 ± 1·63 µM, IC50 amastigotes = 2·80 ± 0·46 and 9·02 ± 5·26 µM, respectively). These results, supported by a lack of toxicity registered over either L929 fibroblasts or primary cultures of cardiomyocytes, confirm that 5-nitroindazolinones 22 and 24 display great selectivity on both drug-sensitive (CL and Tulahuen) and drug-moderately resistant (Y) T. cruzi strains, and therefore, represent an important outcome in the research of Chagas disease chemotherapy.Chagas diseaseTrypanosoma cruzi5-nitroindazolinoneDTUL929 fibroblastsCardiomyocytesDoença de ChagasTrypanosoma cruziMiócitos CardíacosFibroblastosinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; 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| dc.title.pt_BR.fl_str_mv |
Exploring the potential activity spectrum of two 5-nitroindazolinone prototypes on different Trypanosoma cruzi strains |
| title |
Exploring the potential activity spectrum of two 5-nitroindazolinone prototypes on different Trypanosoma cruzi strains |
| spellingShingle |
Exploring the potential activity spectrum of two 5-nitroindazolinone prototypes on different Trypanosoma cruzi strains Fonseca-Berzal, Cristina Chagas disease Trypanosoma cruzi 5-nitroindazolinone DTU L929 fibroblasts Cardiomyocytes Doença de Chagas Trypanosoma cruzi Miócitos Cardíacos Fibroblastos |
| title_short |
Exploring the potential activity spectrum of two 5-nitroindazolinone prototypes on different Trypanosoma cruzi strains |
| title_full |
Exploring the potential activity spectrum of two 5-nitroindazolinone prototypes on different Trypanosoma cruzi strains |
| title_fullStr |
Exploring the potential activity spectrum of two 5-nitroindazolinone prototypes on different Trypanosoma cruzi strains |
| title_full_unstemmed |
Exploring the potential activity spectrum of two 5-nitroindazolinone prototypes on different Trypanosoma cruzi strains |
| title_sort |
Exploring the potential activity spectrum of two 5-nitroindazolinone prototypes on different Trypanosoma cruzi strains |
| author |
Fonseca-Berzal, Cristina |
| author_facet |
Fonseca-Berzal, Cristina Silva, Patricia Bernardino da Silva, Cristiane França Vasconcelos, Mariane Batista, Marcos Meuser Escario, José A. Arán, Vicente J. Gómez-Barrio, Alicia Soeiro, Maria de Nazaré C. |
| author_role |
author |
| author2 |
Silva, Patricia Bernardino da Silva, Cristiane França Vasconcelos, Mariane Batista, Marcos Meuser Escario, José A. Arán, Vicente J. Gómez-Barrio, Alicia Soeiro, Maria de Nazaré C. |
| author2_role |
author author author author author author author author |
| dc.contributor.author.fl_str_mv |
Fonseca-Berzal, Cristina Silva, Patricia Bernardino da Silva, Cristiane França Vasconcelos, Mariane Batista, Marcos Meuser Escario, José A. Arán, Vicente J. Gómez-Barrio, Alicia Soeiro, Maria de Nazaré C. |
| dc.subject.en.pt_BR.fl_str_mv |
Chagas disease Trypanosoma cruzi 5-nitroindazolinone DTU L929 fibroblasts Cardiomyocytes |
| topic |
Chagas disease Trypanosoma cruzi 5-nitroindazolinone DTU L929 fibroblasts Cardiomyocytes Doença de Chagas Trypanosoma cruzi Miócitos Cardíacos Fibroblastos |
| dc.subject.decs.pt_BR.fl_str_mv |
Doença de Chagas Trypanosoma cruzi Miócitos Cardíacos Fibroblastos |
| description |
UCM-UPM & CSIC. CEI Campus Moncloa. Madrid, Spain / Universidad Complutense de Madrid. Facultad de Farmacia. Departamento de Parasitologia. Madrid, Spain. |
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2015 |
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2015 |
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2016-03-22T17:27:09Z |
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2016-03-22T17:27:09Z |
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info:eu-repo/semantics/article |
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FONSECA-BERZAL, Cristina; et al. Exploring the potential activity spectrum of two 5-nitroindazolinone prototypes on different Trypanosoma cruzi strains. Parasitology Open, v.1, e1, 10p, 2015. |
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https://www.arca.fiocruz.br/handle/icict/13247 |
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:10.1017/pao.2015.4 |
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2055-7094 |
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FONSECA-BERZAL, Cristina; et al. Exploring the potential activity spectrum of two 5-nitroindazolinone prototypes on different Trypanosoma cruzi strains. Parasitology Open, v.1, e1, 10p, 2015. :10.1017/pao.2015.4 2055-7094 |
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Cambridge University Press |
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Cambridge University Press |
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