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dc.contributor.author
Gerpe, Alejandra
dc.contributor.author
Boiani Santurio, Lucia
dc.contributor.author
Hernández, Paola
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Sortino, Maximiliano Andrés
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Zacchino, Susana
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González, Mercedes
dc.contributor.author
Cerecetto, Hugo
dc.date.available
2017-03-30T20:29:24Z
dc.date.issued
2010-06
dc.identifier.citation
Gerpe, Alejandra; Boiani Santurio, Lucia; Hernández, Paola; Sortino, Maximiliano Andrés; Zacchino, Susana; et al.; Naftifine-analogues as anti-Trypanosoma cruzi agents; Elsevier Masson; European Journal of Medical Chemistry; 45; 6; 6-2010; 2154-2164
dc.identifier.issn
0223-5234
dc.identifier.uri
http://hdl.handle.net/11336/14562
dc.description.abstract
Chagas disease represents a relevant health problem in Central and South America. The first line of treatment is Nifurtimox and Benznidazole which have a great deal of disadvantages that demands the rapid generation of therapeutic alternatives. Based in our research on aza-thiaheterocycles as anti-Trypanosoma cruzi agents we identified pharmacophores that act through oxidative stress. Here, we describe the synthesis and the activity of new containing bioactive-heterocycles analogues of naftifine as potential T. cruzi membrane sterol biosynthesis inhibitors. Benzimidazole 1,3-dioxides (11 and 13) and quinoxaline 1,4-dioxides (22 and 23) displayed excellent parasite/mammal selectivity indexes. Analysis of the free sterols from parasite incubated with the compounds showed that any of them are able to accumulate squalene suggesting that in the anti-T. cruzi mechanism of action is not involved the inhibition of sterol biosynthesis. Some derivatives were also tested as antifungal agents. The results obtained in the present work open potential therapeutic possibilities of new compounds for these infectious diseases.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Elsevier Masson
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
dc.subject
Alkenylamine
dc.subject
Indazole N-Oxide
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Benzofuroxan
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Benzimidazole 1,3-Dioxide
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Quinoxaline 1,4-Dioxide
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Anti-T. Cruzi Agents
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Química Orgánica
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Ciencias Químicas
dc.subject.classification
CIENCIAS NATURALES Y EXACTAS
dc.title
Naftifine-analogues as anti-Trypanosoma cruzi agents
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2017-03-30T17:43:41Z
dc.journal.volume
45
dc.journal.number
6
dc.journal.pagination
2154-2164
dc.journal.pais
Francia
dc.journal.ciudad
París
dc.description.fil
Fil: Gerpe, Alejandra. Universidad de la República; Uruguay
dc.description.fil
Fil: Boiani Santurio, Lucia. Universidad de la República; Uruguay. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.description.fil
Fil: Hernández, Paola. Universidad de la República; Uruguay
dc.description.fil
Fil: Sortino, Maximiliano Andrés. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Area Farmacognosia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.description.fil
Fil: Zacchino, Susana. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Area Farmacognosia; Argentina
dc.description.fil
Fil: González, Mercedes. Universidad de la República; Uruguay
dc.description.fil
Fil: Cerecetto, Hugo. Universidad de la República; Uruguay
dc.journal.title
European Journal of Medical Chemistry
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0223523410000978
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/j.ejmech.2010.01.052
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