Novel diamides inspired by protein kinase inhibitors as anti-Trypanosoma cruzi agents : in vitro and in vivo evaluations.

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Autor(es): dc.creatorTorchelsen, Fernanda Karoline Vieira da Silva-
Autor(es): dc.creatorPedrosa, Tamiles Caroline Fernandes-
Autor(es): dc.creatorRodrigues, Michelle Peixoto-
Autor(es): dc.creatorAguiar, Alex Ramos de-
Autor(es): dc.creatorOliveira, Fabrício Marques de-
Autor(es): dc.creatorAmarante, Giovanni Wilson-
Autor(es): dc.creatorSales Júnior, Policarpo Ademar Molina-
Autor(es): dc.creatorBranquinho, Renata Tupinambá-
Autor(es): dc.creatorSilva, Sirlaine Pio Gomes da-
Autor(es): dc.creatorSilva, André Talvani Pedrosa da-
Autor(es): dc.creatorMurta, Silvane Maria Fonseca-
Autor(es): dc.creatorMartins, Felipe Terra-
Autor(es): dc.creatorBraun, Rodrigo Ligabue-
Autor(es): dc.creatorTeixeira, Róbson Ricardo-
Autor(es): dc.creatorMosqueira, Vanessa Carla Furtado-
Autor(es): dc.creatorLana, Marta de-
Data de aceite: dc.date.accessioned2025-08-21T15:28:19Z-
Data de disponibilização: dc.date.available2025-08-21T15:28:19Z-
Data de envio: dc.date.issued2025-02-06-
Data de envio: dc.date.issued2025-02-06-
Data de envio: dc.date.issued2022-
Fonte completa do material: dc.identifierhttps://www.repositorio.ufop.br/handle/123456789/19722-
Fonte completa do material: dc.identifierhttps://www.tandfonline.com/doi/full/10.4155/fmc-2023-0090-
Fonte completa do material: dc.identifierhttps://doi.org/10.4155/fmc-2023-0090-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/capes/1015990-
Descrição: dc.descriptionBackground: Chagas disease is a life-threatening illness caused by Trypanosoma cruzi. The involvement of serine-/arginine-rich protein kinase in the T. cruzi life cycle is significant. Aims: To synthesize, characterize and evaluate the trypanocidal activity of diamides inspired by kinase inhibitor, SRPIN340. Material & Methods: Synthesis using a three-step process and characterization by infrared, nuclear magnetic resonance and high-resolution mass spectrometry were conducted. The selectivity index was obtained by the ratio of CC50/IC50 in two in vitro models. The most active compound, 3j, was evaluated using in vitro cytokine assays and assessing in vivo trypanocidal activity. Results: 3j activity in the macrophage J774 lineage showed an anti-inflammatory profile, and mice showed significantly reduced parasitemia and morbidity at low compound dosages. Conclusion: Novel diamide is active against T. cruzi in vitro and in vivo.-
Formato: dc.formatapplication/pdf-
Idioma: dc.languageen-
Direitos: dc.rightsrestrito-
Palavras-chave: dc.subjectChagas disease-
Palavras-chave: dc.subjectDiamides-
Palavras-chave: dc.subjectIn vitro activity-
Palavras-chave: dc.subjectIn vivo activity-
Título: dc.titleNovel diamides inspired by protein kinase inhibitors as anti-Trypanosoma cruzi agents : in vitro and in vivo evaluations.-
Aparece nas coleções:Repositório Institucional - UFOP

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