Please use this identifier to cite or link to this item: https://www.arca.fiocruz.br/handle/icict/10054
Title: In vitro investigation of the efficacy of novel diamidines against Trypanosoma cruzi
Authors: Timm, Bruno Lisboa
Silva, Patrícia Bernardino da
Batista, M. M
Farahat, A. A
Kumar, A
Boykin, D. W
Soeiro, Maria de Nazaré Correia
Affilliation: Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil
Georgia State University. Department of Chemistry. Atlanta, Georgia, USA / Mansoura University. Faculty of Pharmacy. Department of Pharmaceutical Organic Chemistry. Mansoura 35516, Egypt.
Georgia State University. Department of Chemistry. Atlanta, Georgia, USA.
Georgia State University. Department of Chemistry. Atlanta, Georgia, USA.
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil
Abstract: Chagas' disease is a neglected tropical disease caused by Trypanosoma cruzi and constitutes a serious public health problem for Latin America. Its unsatisfactory chemotherapy stimulates the search for novel antiparasitic compounds. Amidines and related compounds exhibit well-known activity towards different microbes including T. cruzi. In this vein, our present aim was to evaluate the biological effect of 10 novel structurally related amidines in vitro against bloodstream and intracellular forms of the parasite as well as their potential toxicity on cardiac cell cultures. Our results show that although active against the extracellular forms, with some of them like DB2247 being 6-fold more effective than benznidazole and displaying very low toxicity (>96 μm), none presented superior trypanocidal effect against intracellular forms as compared with the reference drug. These results may be due to differences in susceptibility profiles related to distinct uptake/extrusion mechanisms and cellular targets between bloodstream and amastigote forms. The present study adds to the knowledge base for the future design of novel amidines that may provide promising activity against T. cruzi.
Keywords: Chagas Disease
Experimental chemotherapy
Aromatic diamidines
keywords: Doença de Chagas
Quimioterapia
Issue Date: 2014
Publisher: Cambridge University Press
Citation: TIMM, B. L et al. In vitro investigation of the efficacy of novel diamidines against Trypanosoma cruzi. Parasitology, n.141, p.1272-1276, 2014.
ISSN: 0031.1820
Embargo date: Sept. 2015
Copyright: restricted access
Appears in Collections:IOC - Artigos de Periódicos

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