Screening of synthetic 1,2,3-triazolic compounds inspired by SRPIN340 as anti-Trypanosoma cruzi agents.

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MetadadosDescriçãoIdioma
Autor(es): dc.creatorTorchelsen, Fernanda Karoline Vieira da Silva-
Autor(es): dc.creatorFernandes, Tamiles Caroline Pedrosa-
Autor(es): dc.creatorSousa, Sara Maria Ribeiro de-
Autor(es): dc.creatorSales Júnior, Policarpo Ademar-
Autor(es): dc.creatorBranquinho, Renata Tupinambá-
Autor(es): dc.creatorMurta, Silvane Maria Fonseca-
Autor(es): dc.creatorTeixeira, Róbson Ricardo-
Autor(es): dc.creatorMosqueira, Vanessa Carla Furtado-
Autor(es): dc.creatorLana, Marta de-
Data de aceite: dc.date.accessioned2025-08-21T15:14:08Z-
Data de disponibilização: dc.date.available2025-08-21T15:14:08Z-
Data de envio: dc.date.issued2025-02-03-
Data de envio: dc.date.issued2025-02-03-
Data de envio: dc.date.issued2023-
Fonte completa do material: dc.identifierhttps://www.repositorio.ufop.br/handle/123456789/19695-
Fonte completa do material: dc.identifierhttps://doi.org/10.1590/0037-8682-0585-2023-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/capes/1007332-
Descrição: dc.descriptionBackground: The current treatments for Chagas disease (CD) include benznidazole and nifurtimox, which have limited efficacy and cause numerous side effects. Triazoles are candidates for new CD treatments due to their ability to eliminate T. cruzi parasites by inhibiting ergosterol synthesis, thereby damaging the cell membranes of the parasite. Methods: Eleven synthetic analogs of the kinase inhibitor SRPIN340 containing a triazole core (compounds 6A-6K) were screened in vitro against the Tulahuen strain transfected with β galactosidase, and their IC50, CC50, and selectivity indexes (SI) were calculated. Compounds with an SI > 50 were further evaluated in mice infected with the T. cruzi Y strain by rapid testing. Results: Eight compounds were active in vitro with IC50 values ranging from 0.5–10.5 μg/mL. The most active compounds, 6E and 6H, had SI values of 125.2 and 69.6, respectively. These compounds also showed in vivo activity, leading to a reduction in parasitemia at doses of 10, 50, and 250 mg/kg/day. At doses of 50 and 250 mg/kg/day, parasitemia was significantly reduced compared to infected untreated animals, with no significant differences between the effects of 6E and 6H.-
Formato: dc.formatapplication/pdf-
Idioma: dc.languageen-
Direitos: dc.rightsaberto-
Direitos: dc.rightsThis is an open access article under the CC BY license. Fonte: PDF do artigo.-
Palavras-chave: dc.subjectChagas disease-
Palavras-chave: dc.subjectTriazoles-
Palavras-chave: dc.subjectScreening-
Palavras-chave: dc.subjectChemotherapy-
Título: dc.titleScreening of synthetic 1,2,3-triazolic compounds inspired by SRPIN340 as anti-Trypanosoma cruzi agents.-
Aparece nas coleções:Repositório Institucional - UFOP

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