@misc{10481/75578,
year = {2022},
month = {5},
url = {http://hdl.handle.net/10481/75578},
abstract = {Amoebas of the genus Acanthamoeba are distributed worldwide, including species with a high pathogenic capacity
for humans. In a similar way to what occurs with other parasitic protozoa, the available treatments show
variable effectiveness in addition to high toxicity, which demands the development of new treatments. Positive
results of 5-nitroindazole derivatives against several protozoa parasites suggest that these compounds may be a
promising tool for the development of efficient antiparasitic drugs. In the present work we have evaluated the in
vitro activity of ten 5-nitroindazole derivatives against Acanthamoeba castellanii trophozoites and cysts. To that
end, AlamarBlue Assay Reagent® was used to determine the activity against trophozoites compared to the
reference drug chlorhexidine digluconate. Cytotoxicity of the compounds was evaluated using Vero cells. The
activity on cysts was evaluated by light microscopy and using a Neubauer chamber to quantifying cysts and
presence of trophozoites, as an indication of cyst. Our results showed the effectiveness of the 5-nitroindazole
derivatives tested against both trophozoites and cysts of A. castellani highlighting 5-nitroindazole derivative 8
which showed a 80% activity on cysts, which is higher than that of the reference drug. Moreover, 5-nitroindazole
derivatives 8, 9 and 10 were more effective on trophozoites than the reference drug showing IC50 values lower
than 5 μM. Taking together these results, these 5-nitroindazole derivatives specially compound 8, might be a
promising alternative for the development of more efficient treatments against A. castellani infection.},
organization = {FEDER funds of the E.U	CTQ2013-14892	
2010-CSD2010-00065},
organization = {Unidad de Excelencia MDM	2015-0038},
organization = {Center for Forestry Research & Experimentation (CIEF)},
organization = {European Commission	PROMETEO II 2015-002},
organization = {Alfonso Martin Escudero Foundation},
organization = {Spanish Government},
publisher = {Elsevier},
keywords = {Acanthamoeba castellanii},
keywords = {Amoebicidal},
keywords = {Chlorhexidine digluconate},
keywords = {5-nitroindazole derivatives},
title = {5-Nitroindazole derivatives as potential therapeutic alternatives against Acanthamoeba castellanii},
doi = {10.1016/j.actatropica.2022.106538},
author = {Martín Escolano, Rubén and Pérez Cordón, Gregorio and Marín Sánchez, Clotilde and Sánchez Moreno, Manuel and Rosales Lombardo, María José},
}