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In vitro and in vivo biological effects of novel arylimidamide derivatives against Trypanosoma cruzi. | LitMetric

AI Article Synopsis

  • - Chagas disease (CD), caused by the parasite Trypanosoma cruzi, poses a significant health threat in Latin America, and existing treatments are often ineffective and have side effects.
  • - The study investigated eight novel aromatic diamidines and arylimidamides (AIAs) for their effects on T. cruzi, finding that two compounds, 18SAB075 and 16DAP002, had promising activity against different parasite strains without harming host cells.
  • - Although 18SAB075 showed potential in reducing parasitemia and providing some protection in acute infection models, its effectiveness was still lower than that of the standard treatment, benznidazole.

Article Abstract

Chagas disease (CD), a neglected tropical disease caused by Trypanosoma cruzi, remains a serious public health problem in several Latin American countries. The available chemotherapies for CD have limited efficacy and exhibit undesirable side effects. Aromatic diamidines and arylimidamides (AIAs) have shown broad-spectrum activity against intracellular parasites, including T. cruzi. Therefore, our aim was to evaluate the biological activity of eight novel AIAs (16DAP002, 16SAB079, 18SAB075, 23SMB022, 23SMB026, 23SMB054, 26SMB070, and 27SMB009) against experimental models of T. cruzi infection in vitro and in vivo. Our data show that none of the compounds induced a loss of cellular viability up to 32 μM. Two AIAs, 18SAB075 and 16DAP002, exhibited good in vitro activity against different parasite strains (Y and Tulahuen) and against the two relevant forms of the parasite for mammalian hosts. Due to the excellent selective indexes of 18SAB075, this AIA was moved to in vivo tests for acute toxicity and parasite efficacy; nontoxic doses (no-observed-adverse-effect level [NOAEL], 50 mg/kg) were employed in the tests for parasite efficacy. In experimental models of acute T. cruzi infection, 18SAB075 reduced parasitemia levels only up to 50% and led to 40% protection against mortality (at 5 mg/kg of body weight), being less effective than the reference drug, benznidazole.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4068584PMC
http://dx.doi.org/10.1128/AAC.02353-14DOI Listing

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