| Author | Capelini, Camila | |
| Author | Souza, Kátia R. de | |
| Author | Barbosa, Juliana M. C. | |
| Author | Sales Junior, Policarpo Ademar | |
| Author | Murta, Silvane Maria Fonseca | |
| Author | Wardell, Solange M. S. V. | |
| Author | Wardell, James L. | |
| Author | Silva, Edson F. da | |
| Author | Carvalho, Samir A. | |
| Access date | 2022-12-16T12:31:19Z | |
| Available date | 2022-12-16T12:31:19Z | |
| Document date | 2021 | |
| Citation | CAPELINI, Camila et al. Phenoxyacetohydrazones against Trypanosoma cruzi. Med Chem Res., v. 30, n. 9, p. 1703–1712, 2021. doi.org/10.1007/s00044-021-02768-9 | en_US |
| ISSN | 054-2523 | en_US |
| URI | https://www.arca.fiocruz.br/handle/icict/55996 | |
| Language | eng | en_US |
| Publisher | Springer | en_US |
| Rights | restricted access | |
| Title | Phenoxyacetohydrazones against Trypanosoma cruzi | en_US |
| Type | Article | |
| Abstract | Herein, we reported the design, synthesis, antitrypanosomal and cytotoxic evaluation of a new phenoxyacetohydrazones series. All derivatives were assayed against bloodstream trypomastigote forms of T. cruzi (Y strain) and intracellular amastigotes using the model of L-929 cells infected with trypomastigotes of the Tulahuen strain. Compound (E)-N′-(3.4-dihydroxybenzylidene)-2-phenoxyacetohydrazide (11) showed activity against trypomastigotes (IC50/24 h = 10.3 µM) equivalent to that of benznidazole and with selectivity index (SI) = 46. Against infected cultures, (E)-N′-((5-nitrofuran-2-yl) methylene)-2-phenoxyacetohydrazide (19) was active at the nanomolar range (IC50/96 h = 40 nM), being about 38-fold more active than the standard drug and with SI equal to 2500. Thus, derivatives 11 and 19 could be considered a good prototypes for the development of new candidates for Chagas disease therapy. | en_US |
| Affilliation | Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos—Farmanguinhos. Rio de Janeiro, RJ, Brazil/Instituto Militar de Engenharia. Seção de Engenharia Química. Laboratório de Físico-Química de Materiais. Rio de Janeiro, Brazil | en_US |
| Affilliation | Instituto Militar de Engenharia. Seção de Engenharia Química. Laboratório de Físico-Química de Materiais. Rio de Janeiro, Brazil | en_US |
| Affilliation | Laboratório de Biologia Celular, Instituto Oswaldo Cruz, Fundação Oswaldo Cruz, 21040-900, Rio de Janeiro, RJ, Brazil | en_US |
| Affilliation | Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brazil | en_US |
| Affilliation | Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brazil | en_US |
| Affilliation | CHEMSOL, 1 Harcourt Road. Aberdeen, AB15 5NY, Scotland | en_US |
| Affilliation | Department of Chemistry. University of Aberdeen. Old Aberdeen, AB24 3UE, Scotland | en_US |
| Affilliation | Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos—Farmanguinhos. Rio de Janeiro, RJ, Brazil | en_US |
| Affilliation | Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos—Farmanguinhos. Rio de Janeiro, RJ, Brazil | en_US |
