Benznidazole biotransformation in rat heart microsomal fraction without observable ultrastructural alterations: comparison to Nifurtimox-induced cardiac effects

Mecca, María Montalto de; Bartel, Laura C.; Castro, Clementina; Castro, J.A.

doi:10.1590/s0074-02762008000600007

Cited by 25 publications

(15 citation statements)

References 19 publications

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“…Conversely, toxicity has been described in other tissues (de Mecca et al 2008). For instance, an increased risk of lymphomas was found in experimental animals (Teixeira et al 1990).…”

Section: Tolerance and Adherencementioning

confidence: 99%

Therapy, diagnosis and prognosis of chronic Chagas disease: insight gained in Argentina

Sosa-Estáni

Viotti²,

Segura

2009

Mem. Inst. Oswaldo Cruz

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“…Conversely, toxicity has been described in other tissues (de Mecca et al 2008). For instance, an increased risk of lymphomas was found in experimental animals (Teixeira et al 1990).…”

Section: Tolerance and Adherencementioning

confidence: 99%

Therapy, diagnosis and prognosis of chronic Chagas disease: insight gained in Argentina

Sosa-Estáni

Viotti²,

Segura

2009

Mem. Inst. Oswaldo Cruz

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“…Other types of side effects include reversible clastogenesis and mutagenesis with benznidazole and nifurtimox without any associated manifestations [55, 56], toxicity against other tissues [57] or increased risk of lymphomas in experimental animals [58] have been described, but never demonstrated among a general population of infected patients undergoing treatment [59] and never played a role in animal models [60]. Adequate management of side effects is necessary to carry out treatment as well as to diminish unfounded fears with the use of trypanocidal drugs [53, 61].…”

Section: Resultsmentioning

confidence: 99%

Therapy of Chagas Disease: Implications for Levels of Prevention

Sosa-Estáni

Colantonio

Segura

2012

Journal of Tropical Medicine

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This paper reviews the evidence supporting the use of etiological treatment for Chagas disease that has changed the standard of care for patients withTrypanosoma cruziinfection in the last decades. Implications of this evidence on different levels of prevention as well as gaps in current knowledge are also discussed. In this regard, etiological treatment has shown to be beneficial as an intervention for secondary prevention to successfully cure the infection or to delay, reduce, or prevent the progression to disease, and as primary disease prevention by breaking the chain of transmission. Timely diagnosis during initial stages would allow for the prescription of appropriate therapies mainly in the primary health care system thus improving chances for a better quality of life. Based on current evidence, etiological treatment has to be considered as an essential public health strategy useful to reduce disease burden and to eliminate Chagas disease altogether.

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“…5A and B) (10). Additionally, thiazole 4, unlike Bnz and Nfx (see Table S3) (6,28,29), was not mutagenic in the Ames test against the five strains recommended by the OECD, was not genotoxic in vivo at the assayed dose, and possessed a high LD 50 .…”

Section: Discussionmentioning

confidence: 96%

Identification of a New Amide-Containing Thiazole as a Drug Candidate for Treatment of Chagas' Disease

Álvarez

Varela

Cruces

et al. 2015

Antimicrob Agents Chemother

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Although the parasitic infection Chagas' disease was described over 100 years ago, even now there are not suitable drugs. The available drugs nifurtimox and benznidazole have limited efficacies and tolerances, with proven mutagenic effects. Attempting to find appropriate drugs to deal with this problem, here we report on the development and pharmacological characterization of new amide-containing thiazoles. In the present study, we evaluated the in vitro and in vivo effects of new candidates against Trypanosoma cruzi, the etiological agent of Chagas' disease. The lead amide-containing thiazole derivative had potent in vitro activity, an absence of both in vitro mutagenic and in vivo clastogenic effects, and excellent in vitro selectivity and in vivo tolerance. The compound suppressed parasitemia in mice, modifying the anti-T. cruzi antibodies like the reference drug, benznidazole, and displayed the lowest mortality among the tested drugs. The present evidence suggests that this compound is a promising anti-T. cruzi agent surpassing the lead optimization stage in drug development and leading to a candidate for preclinical study.

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Benznidazole biotransformation in rat heart microsomal fraction without observable ultrastructural alterations: comparison to Nifurtimox-induced cardiac effects

Abstract: Benznidazole (Bz) and Nifurtimox (Nfx)

Cited by 25 publications

References 19 publications

Therapy, diagnosis and prognosis of chronic Chagas disease: insight gained in Argentina

Therapy, diagnosis and prognosis of chronic Chagas disease: insight gained in Argentina

Therapy of Chagas Disease: Implications for Levels of Prevention

Identification of a New Amide-Containing Thiazole as a Drug Candidate for Treatment of Chagas' Disease

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