Author | Gomes, Paulo André Teixeira de Moraes | |
Author | Oliveira, Arsênio Rodrigues | |
Author | Cardoso, Marcos Veríssimo de Oliveira | |
Author | Santiago, Edna de Farias | |
Author | Barbosa, Miria de Oliveira | |
Author | Siqueira, Lucianna Rabelo Pessoa de | |
Author | Moreira, Diogo Rodrigo Magalhães | |
Author | Bastos, Tanira Matutino | |
Author | Brayner, Fabio Andre | |
Author | Soares, Milena Botelho Pereira | |
Author | Oliveira Mendes, Andresa Pereira de | |
Author | Castro, Maria Carolina Accioly Brelaz de | |
Author | Pereira, Valeria Rego Alves | |
Author | Leite, Ana Cristina Lima | |
Access date | 2016-05-13T17:31:23Z | |
Available date | 2016-05-13T17:31:23Z | |
Document date | 2016 | |
Citation | GOMES, P. A. T. M. et al. Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi. European Journal of Medicinal Chemistry , v. 111, p.46-57, 2016. | pt_BR |
ISSN | 0223-5234 | |
URI | https://www.arca.fiocruz.br/handle/icict/14267 | |
Language | eng | pt_BR |
Publisher | Elsevier | pt_BR |
Rights | open access | pt_BR |
Title | Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi. | pt_BR |
Type | Article | pt_BR |
DOI | /dx.doi.org/10.1016/j.ejmech.2016.01.010 | |
Abstract | Chagas disease is a parasitic infection caused by protozoan Trypanosoma cruzi that affects approximately
6e7 million people worldwide. Benznidazole is the only drug approved for treatment during the acute
and asymptomatic chronic phases; however, its efficacy during the symptomatic chronic phase is
controversial. The present work reports the synthesis and anti-T. cruzi activities of a novel series of
phthalimido-thiazoles. Some of these compounds showed potent inhibition of the trypomastigote form
of the parasite at low cytotoxicity concentrations in spleen cells, and the resulting structure-activity
relationships are discussed. We also showed that phthalimido-thiazoles induced ultrastructural alterations
on morphology, flagellum shortening, chromatin condensation, mitochondria swelling, reservosomes
alterations and endoplasmic reticulum dilation. Together, these data revealed, for the first time, a
novel series of phthalimido-thiazoles-structure-based compounds with potential effects against T. cruzi
and lead-like characteristics against Chagas disease. | pt_BR |
Affilliation | Universidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Centro de Ciências da Saúde. Recife, PE, Brasil | pt_BR |
Affilliation | Universidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Centro de Ciências da Saúde. Recife, PE, Brasil | pt_BR |
Affilliation | Universidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Centro de Ciências da Saúde. Recife, PE, Brasil | pt_BR |
Affilliation | Universidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Centro de Ciências da Saúde. Recife, PE, Brasil | pt_BR |
Affilliation | Universidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Centro de Ciências da Saúde. Recife, PE, Brasil | pt_BR |
Affilliation | Universidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Centro de Ciências da Saúde. Recife, PE, Brasil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
Affilliation | Laboratório de Imunologia Keizo Asami-LIKA/UFPE. Recife, PE, Brasil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil / Hospital São Rafael. Centro de Biotecnologia e Terapia Celular. Salvador BA, Brasil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Recife, PE, Brasil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Recife, PE, Brasil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Recife, PE, Brasil | pt_BR |
Affilliation | Universidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Centro de Ciências da Saúde. Recife, PE, Brasil | pt_BR |
Subject | Chagas disease | pt_BR |
Subject | Trypanosoma cruzi | pt_BR |
Subject | Thiazole | pt_BR |
Subject | Hydrazone | pt_BR |
Subject | Phthalimide | pt_BR |