In vitro activity of Etanidazole against the protozoan parasite Trypanosoma cruzi

Petray, Patricia; Morilla, María José; Corral, Ricardo S.; Romero, Eder Lilia

doi:10.1590/s0074-02762004000200021

Cited by 16 publications

(8 citation statements)

References 9 publications

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“…Statistical analysis -The cytotoxicity percentage (CP) against Vero cells and the activity percentages (AP) against epimastigotes and amastigotes were calculated using the following formula: AP (or CP) = (1-Mt/ Mc)*100 , Sánchez et al 2002, Petray et al 2004, where Mt represents the measurement taken after the treatment and Mc is the measurement of the negative control. Each concentration of the compounds was assayed in triplicate on the same day and the assays were repeated at least three times on different days.…”

Section: Methodsmentioning

confidence: 99%

“…Each concentration of the compounds was assayed in triplicate on the same day and the assays were repeated at least three times on different days. The IC 50 value for each compound was calculated by plotting the AP (or CP) against the logarithm of the com- pound concentration for each assay (Petray et al 2004). Comparisons of the mean IC 50 values were made using the one-tailed ANOVA with the Tukey test as a post-hoc test.…”

Section: Methodsmentioning

confidence: 99%

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In vitro activity of thienyl-2-nitropropene compounds against Trypanosoma cruzi

Herrera

Vallejos

Loaiza

et al. 2009

Mem. Inst. Oswaldo Cruz

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Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

In vitro activity of thienyl-2-nitropropene compounds against Trypanosoma cruzi

Herrera

Vallejos

Loaiza

et al. 2009

Mem. Inst. Oswaldo Cruz

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“…Nitroimidazoles are prodrugs that are activated by a variety of reductases (Quon et al ., 1992; Melo et al ., 2000; Singh et al ., 2008) to the corresponding hydroxylamino and/or nitroso derivatives, which in turn react with intracellular nucleophiles including DNA (Barry et al ., 2004; Nagasawa et al ., 2006). They are particularly useful for drug‐resistant Mycobacterium tuberculosis (Barry et al ., 2004; Khan et al ., 2008), treatment of Chagas' disease (Petray et al ., 2004; Garcia et al ., 2005), and as radiosensitizers for tumour therapy (Nagasawa et al ., 2006).…”

Section: Introductionmentioning

confidence: 99%

Catabolic pathway for 2‐nitroimidazole involves a novel nitrohydrolase that also confers drug resistance

Spain

2011

Environmental Microbiology

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Antibiotic resistance in pathogens can be mediated by catabolic enzymes thought to originate from soil bacteria, but the physiological functions and evolutionary origins of the enzymes in natural ecosystems are poorly understood. 2-Nitroimidazole (2NI) is a natural antibiotic and an analogue of the synthetic nitroimidazoles used for treatment of tuberculosis, Chagas' disease and cancer. Mycobacterium sp. JS330 was isolated from soil based on its ability to use 2NI as a sole growth substrate. The initial step in the degradation pathway is the hydrolytic denitration of 2NI to produce imidazol-2-one and nitrite. The amino acid sequence of 2NI nitrohydrolase is highly divergent from those of biochemically characterized enzymes, and it confers drug resistance when it is heterologously expressed in Escherichia coli. The unusual enzymatic reaction seems likely to determine the flux of nitroimidazole in natural ecosystems and also represents the discovery of a previously unreported drug resistance mechanism in soil before its identification in clinical situations.

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“…5-nitroimidazole derivatives have been tested in cell-based assays and in enzyme assays against HIV-1 recombinant reverse transcriptase [9,10]. 2-Nitroimidazoles play a major role as bioreductive markers for tumour hypoxia, as radiosensitizers [11][12][13], and some also demonstrate antiprotozoan activity [14]. Some dinitro and mono nitroimidazole derivatives have been predicted as notable radiosensitizers, antiprotozoal and antibacterial or antiepileptic agents [15].…”

Section: Introductionmentioning

confidence: 99%

Synthetic Nitroimidazoles: Biological Activities and Mutagenicity Relationships

Mital

2009

Sci. Pharm.

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Parasitic and bacterial infections affecting the gastrointestinal tract represent a significant cause of morbidity and mortality worldwide. Nitroheterocyclic drugs have been available since the early 1960s for the treatment of anaerobic protozoa. The application of these drugs has widened and they are presently used to treat anaerobic pathogenic bacteria and protozoa. 5-nitroimidazoles are a well-established group of antiprotozoal and antibacterial agents that inhibit the growth of both anaerobic bacteria and certain anaerobic protozoa, such as Trichomonas vaginalis, Entamoeba histolytica and Giardia lamblia. The important antibacterial and antiprotozoal activities of nitroimidazoles are associated with reductive metabolism that has led to considerable interest in nitroimidazole reduction chemistry and the synthesis of new, highly effective drugs. The present review provides a brief account of various biological activities exhibited by synthetic nitroimidazole derivatives as well as their structure-mutagenicity relationships.

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In vitro activity of Etanidazole against the protozoan parasite Trypanosoma cruzi

Cited by 16 publications

References 9 publications

In vitro activity of thienyl-2-nitropropene compounds against Trypanosoma cruzi

In vitro activity of thienyl-2-nitropropene compounds against Trypanosoma cruzi

Catabolic pathway for 2‐nitroimidazole involves a novel nitrohydrolase that also confers drug resistance

Synthetic Nitroimidazoles: Biological Activities and Mutagenicity Relationships

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