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

Página do item simplificado
dc.creatorTorchelsen, Fernanda Karoline Vieira da Silva
dc.creatorPedrosa, Tamiles Caroline Fernandes
dc.creatorRodrigues, Michelle Peixoto
dc.creatorAguiar, Alex Ramos de
dc.creatorOliveira, Fabricio Marques de
dc.creatorAmarante, Giovanni Wilson
dc.creatorSales Junior, Policarpo Ademar
dc.creatorBranquinho, Renata Tupinambá
dc.creatorSilva, Sirlaine Pio Gomes da
dc.creatorSilva, Andre Talvani Pedrosa da
dc.creatorMurta, Silvane Maria Fonseca
dc.creatorMartins, Felipe Terra
dc.creatorSilva, Andre Talvani Pedrosa da
dc.date.accessioned2023-11-10T12:29:23Z
dc.date.available2023-11-10T12:29:23Z
dc.date.issued2023-08-31
dc.description.abstractBackground: 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. cruziin vitro and in vivo.
dc.identifier.citationTORCHELSEN, Fernanda Karoline Vieira da Silva et al. Novel diamides inspired by protein kinase inhibitors as anti-Trypanosoma cruzi agents: in vitro and in vivo evaluations. Future Medicinal Chemistry, London, v. 15, n. 16, p. 1469-1489, 2023. DOI: 10.4155/fmc-2023-0090. Disponível em: https://www.future-science.com/doi/10.4155/fmc-2023-0090. Acesso em: 6 nov. 2023.
dc.identifier.doi10.4155/fmc-2023-0090
dc.identifier.issn1756-8919
dc.identifier.issne- 1756-8927
dc.identifier.urihttps://www.future-science.com/doi/10.4155/fmc-2023-0090
dc.language.isoeng
dc.publisher.countryGra-bretanha
dc.publisher.departmentInstituto de Química - IQ (RMG)
dc.rightsAcesso Restrito
dc.subjectChagas disease
dc.subjectDiamides
dc.subjectIn vitro activity
dc.subjectIn vivo activity
dc.subjectSRPIN340
dc.subjectTrypanosoma cruzi
dc.titleNovel diamides inspired by protein kinase inhibitors as anti-Trypanosoma cruzi agents: in vitro and in vivo evaluations
dc.typeArtigo

Arquivos

Licença do Pacote
Agora exibindo 1 - 1 de 1
Nenhuma Miniatura disponível
Nome:
license.txt
Tamanho:
1.71 KB
Formato:
Item-specific license agreed upon to submission
Descrição:
Baixar

Coleções

IQ - Artigos publicados em periódicos