In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of a Novel Nitro-derivative
Nitroarylidenemalononitriles and their cyanoacetamide derivatives with remarkable anti-epimastigote properties, were synthesized attempting to obtain new 3,5-diamino-4-(5'-nitroarylidene)-4H-thiadiazine 1,1-dioxide derivatives, which in previous reports had shown anti-Trypanosoma cruzi activity...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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Fundação Oswaldo Cruz (FIOCRUZ)
2002-06-01
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| Series: | Memorias do Instituto Oswaldo Cruz |
| Subjects: | |
| Online Access: | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762002000400019 |
| _version_ | 1797721326567292928 |
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| author | Susana Muelas-Serrano Ana Le-Senne Carlos Fernández-Portillo Juan José Nogal Carmen Ochoa Alicia Gómez-Barrio |
| author_facet | Susana Muelas-Serrano Ana Le-Senne Carlos Fernández-Portillo Juan José Nogal Carmen Ochoa Alicia Gómez-Barrio |
| author_sort | Susana Muelas-Serrano |
| collection | DOAJ |
| description | Nitroarylidenemalononitriles and their cyanoacetamide derivatives with remarkable anti-epimastigote properties, were synthesized attempting to obtain new 3,5-diamino-4-(5'-nitroarylidene)-4H-thiadiazine 1,1-dioxide derivatives, which in previous reports had shown anti-Trypanosoma cruzi activity. Tests to evaluate the cytotoxicity of compounds were performed on J774 macrophages. 5-nitro-2-thienyl-malononitrile (5NO2TM), was the only product which maintained a high anti-epimastigote activity at concentrations in which it was no longer cytotoxic, thus it was assayed against intracellular amastigotes. Its anti-amastigote activity was similar to that of nifurtimox. Afterwards in vivo toxicity and anti-chagasic activity were determined. A reduction in parasitemia was observed. |
| first_indexed | 2024-03-12T09:31:49Z |
| format | Article |
| id | doaj.art-0ae5da67da4f43f78c11c8f57d93e43b |
| institution | Directory Open Access Journal |
| issn | 0074-0276 1678-8060 |
| language | English |
| last_indexed | 2024-03-12T09:31:49Z |
| publishDate | 2002-06-01 |
| publisher | Fundação Oswaldo Cruz (FIOCRUZ) |
| record_format | Article |
| series | Memorias do Instituto Oswaldo Cruz |
| spelling | doaj.art-0ae5da67da4f43f78c11c8f57d93e43b2023-09-02T13:53:50ZengFundação Oswaldo Cruz (FIOCRUZ)Memorias do Instituto Oswaldo Cruz0074-02761678-80602002-06-0197455355710.1590/S0074-02762002000400019In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of a Novel Nitro-derivativeSusana Muelas-SerranoAna Le-SenneCarlos Fernández-PortilloJuan José NogalCarmen OchoaAlicia Gómez-BarrioNitroarylidenemalononitriles and their cyanoacetamide derivatives with remarkable anti-epimastigote properties, were synthesized attempting to obtain new 3,5-diamino-4-(5'-nitroarylidene)-4H-thiadiazine 1,1-dioxide derivatives, which in previous reports had shown anti-Trypanosoma cruzi activity. Tests to evaluate the cytotoxicity of compounds were performed on J774 macrophages. 5-nitro-2-thienyl-malononitrile (5NO2TM), was the only product which maintained a high anti-epimastigote activity at concentrations in which it was no longer cytotoxic, thus it was assayed against intracellular amastigotes. Its anti-amastigote activity was similar to that of nifurtimox. Afterwards in vivo toxicity and anti-chagasic activity were determined. A reduction in parasitemia was observed.http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762002000400019Trypanosoma cruzinitroarylidenemalononitrilesin vitro assayscytotoxicity assaysin vivo experiments |
| spellingShingle | Susana Muelas-Serrano Ana Le-Senne Carlos Fernández-Portillo Juan José Nogal Carmen Ochoa Alicia Gómez-Barrio In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of a Novel Nitro-derivative Memorias do Instituto Oswaldo Cruz Trypanosoma cruzi nitroarylidene malononitriles in vitro assays cytotoxicity assays in vivo experiments |
| title | In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of a Novel Nitro-derivative |
| title_full | In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of a Novel Nitro-derivative |
| title_fullStr | In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of a Novel Nitro-derivative |
| title_full_unstemmed | In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of a Novel Nitro-derivative |
| title_short | In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of a Novel Nitro-derivative |
| title_sort | in vitro and in vivo anti trypanosoma cruzi activity of a novel nitro derivative |
| topic | Trypanosoma cruzi nitroarylidene malononitriles in vitro assays cytotoxicity assays in vivo experiments |
| url | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762002000400019 |
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