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In vitro assessment of 3-alkoxy-5-nitroindazole-derived ethylamines and related compounds as potential antileishmanial drugs. | LitMetric

In vitro assessment of 3-alkoxy-5-nitroindazole-derived ethylamines and related compounds as potential antileishmanial drugs.

Bioorg Chem

Departamento de Parasitología, Instituto de Investigación Biosanitaria (ibs.Granada), Hospitales Universitarios de Granada, Universidad de Granada, c/ Severo Ochoa s/n, 18071 Granada, Spain. Electronic address:

Published: November 2019

AI Article Synopsis

  • * Researchers tested 12 different 5-nitroindazole derivatives, which showed low toxicity in macrophages and higher effectiveness against Leishmania parasites than the standard drug Meglumine Antimoniate (Glucantime®).
  • * The study found that these new compounds not only demonstrated better leishmanicidal effects but also provided insights into their action mechanisms, encouraging further research, including in vivo studies, to explore their potential.

Article Abstract

Leishmaniasis is a widespread neglected tropical disease complex that is responsible of one million new cases per year. Current treatments are outdated and pose many problems that new drugs need to overcome. With the goal of developing new, safe, and affordable drugs, we have studied the in vitro activity of 12 different 5-nitroindazole derivatives that showed previous activity against different strains of Trypanosoma cruzi in a previous work. T. cruzi belongs to the same family as Leishmania spp., and treatments for the disease it produces also needs renewal. Among the derivatives tested, compounds 1, 2, 9, 10, 11, and 12 showed low J774.2 macrophage toxicity, while their effect against both intracellular and extracellular forms of the studied parasites was higher than the ones found for the reference drug Meglumine Antimoniate (Glucantime®). In addition, their Fe-SOD inhibitory effect, the infection rates, metabolite alteration, and mitochondrial membrane potential of the parasites treated with the selected drugs were studied in order to gain insights into the action mechanism, and the results of these tests were more promising than those found with glucantime, as the leishmanicidal effect of these new drug candidates was higher. The promising results are encouraging to test these derivatives in more complex studies, such as in vivo studies and other experiments that could find out the exact mechanism of action.

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Source
http://dx.doi.org/10.1016/j.bioorg.2019.103274DOI Listing

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