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dc.contributor.author
Gerpe, Alejandra
dc.contributor.author
Alvarez, Guzmán
dc.contributor.author
Benítez, Diego
dc.contributor.author
Boiani, Lucía
dc.contributor.author
Quiroga, Martín
dc.contributor.author
Hernández, Paola
dc.contributor.author
Sortino, Maximiliano Andrés
dc.contributor.author
Zacchino, Susana Alicia Stella
dc.contributor.author
González, Mercedes
dc.contributor.author
Cerecetto, Hugo
dc.date.available
2021-04-16T18:04:30Z
dc.date.issued
2009-11
dc.identifier.citation
Gerpe, Alejandra; Alvarez, Guzmán; Benítez, Diego; Boiani, Lucía; Quiroga, Martín; et al.; 5-Nitrofuranes and 5-nitrothiophenes with anti-Trypanosoma cruzi activity and ability to accumulate squalene; Pergamon-Elsevier Science Ltd; Bioorganic & Medicinal Chemistry; 17; 21; 11-2009; 7500-7509
dc.identifier.issn
0968-0896
dc.identifier.uri
http://hdl.handle.net/11336/130232
dc.description.abstract
Chagas disease represents a serious public health problem in South America. The first line of treatment is Nifurtimox and Benznidazole which generate toxic effects in treated patients. We have recently shown that a number of 5-nitrofuranes possess activity against Trypanosoma cruzi through oxidative stress and inhibition of parasite ergosterol biosynthesis, specifically at the level of squalene epoxidase. Here, we identify new 5-nitrofuranes and the thia-analogues with excellent effects on the viability of T. cruzi and adequate parasite/mammal selectivity indexes. Analysis of the free sterols from parasite incubated, during 120 h, with the compounds showed that some of them accumulated squalene suggesting the squalene epoxidase activity inhibition of the parasite. Nifurtimox was able to accumulate squalene only at lower incubation times. Due to this fact some derivatives were also tested as antifungal agents. Quantitative structure-activity relationship studies were also performed showing relevant features for further new derivatives design. Taken together, the results obtained in the present work point to a more general effect of 5-nitrofuranes and 5-nitrothiophenes in trypanosomatids, opening potential therapeutic possibilities of them for these infectious diseases.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Pergamon-Elsevier Science Ltd
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
5-NITROTHIOPHENE
dc.subject
8-NITROFURAN
dc.subject
ANTI-TRYPANOSOMA CRUZI COMPOUNDS
dc.subject
SQUALENE EPOXIDASE
dc.subject
STEROL BIOSYNTHESIS INHIBITORS
dc.subject.classification
Química Orgánica
dc.subject.classification
Ciencias Químicas
dc.subject.classification
CIENCIAS NATURALES Y EXACTAS
dc.title
5-Nitrofuranes and 5-nitrothiophenes with anti-Trypanosoma cruzi activity and ability to accumulate squalene
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2020-07-22T15:43:04Z
dc.journal.volume
17
dc.journal.number
21
dc.journal.pagination
7500-7509
dc.journal.pais
Estados Unidos
dc.description.fil
Fil: Gerpe, Alejandra. Universidad de la República; Uruguay
dc.description.fil
Fil: Alvarez, Guzmán. Universidad de la República; Uruguay
dc.description.fil
Fil: Benítez, Diego. Universidad de la República; Uruguay
dc.description.fil
Fil: Boiani, Lucía. Universidad de la República; Uruguay
dc.description.fil
Fil: Quiroga, Martín. No especifíca;
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; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; Argentina
dc.description.fil
Fil: Zacchino, Susana Alicia Stella. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; 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
Bioorganic & Medicinal Chemistry
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/abs/pii/S0968089609008657
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/j.bmc.2009.09.013
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