2023
DOI: 10.3390/biom13040637
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Further Investigations of Nitroheterocyclic Compounds as Potential Antikinetoplastid Drug Candidates

Abstract: Due to the lack of specific vaccines, management of the trypanosomatid-caused neglected tropical diseases (sleeping sickness, Chagas disease and leishmaniasis) relies exclusively on pharmacological treatments. Current drugs against them are scarce, old and exhibit disadvantages, such as adverse effects, parenteral administration, chemical instability and high costs which are often unaffordable for endemic low-income countries. Discoveries of new pharmacological entities for the treatment of these diseases are … Show more

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Cited by 10 publications
(11 citation statements)
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“…Of these, approximately 50,000 to 90,000 are VL, and 600,000 to 1 million are various forms of CL and MCL. The annual death toll from leishmaniasis disease is between 26,000 and 65,000 [23,24]. Additionally, the economic impact per year has been estimated at 1.4 million Disability-Adjusted Life Years (DALYs), primarily associated with VL [8].…”
Section: -Nitroimidazole Derivatives With Anti-leishmanial Activitymentioning
confidence: 99%
“…Of these, approximately 50,000 to 90,000 are VL, and 600,000 to 1 million are various forms of CL and MCL. The annual death toll from leishmaniasis disease is between 26,000 and 65,000 [23,24]. Additionally, the economic impact per year has been estimated at 1.4 million Disability-Adjusted Life Years (DALYs), primarily associated with VL [8].…”
Section: -Nitroimidazole Derivatives With Anti-leishmanial Activitymentioning
confidence: 99%
“…Sleeping sickness is currently being treated with the combination therapy NECT, comprising nifurtimox and the ornithine analog α-difluoromethylornithine (DFMO; eflornithine) (Figure 1), and recently, fexinidazole has been successfully included [17]. For Chagas disease, the nitroheterocycles nifurtimox and benznidazole have been the two drugs of choice for several decades with good results [18].…”
Section: Introductionmentioning
confidence: 99%

Polyamine Metabolism for Drug Intervention in Trypanosomatids

Pérez-Pertejo,
García-Estrada,
Martínez-Valladares
et al. 2024
Pathogens
Self Cite
“…The potential toxicity phenomena associated with nitroheterocycles limited their use and even prohibited their inclusion in drug discovery programs. Nevertheless, the urgent need for novel trypanocidal agents and the approval of fexinidazole have led to renewed interest in these scaffolds …”
Section: Introductionmentioning
confidence: 99%
“…However, caution is advised not to develop too many nitroheterocycles against trypanosomatid diseases at once because the high dependency on prodrug activation by nitroreductase I can lead to drug resistance; thus, it is essential to determine the activation mechanism of new nitroheterocyclic compounds in the early stage of drug discovery …”
Section: Introductionmentioning
confidence: 99%
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