English   español  
Please use this identifier to cite or link to this item: http://hdl.handle.net/10261/117670
Share/Impact:
Statistics
logo share SHARE logo core CORE   Add this article to your Mendeley library MendeleyBASE

Visualizar otros formatos: MARC | Dublin Core | RDF | ORE | MODS | METS | DIDL
Exportar a otros formatos:
Title

In vitro leishmanicidal activity of 1,3-disubstituted 5-nitroindazoles

AuthorsMarín, C.; Ramírez-Macías, Inmaculada; Rosales, María José; Muro, Beatriz; Reviriego, Felipe ; Navarro, Pilar ; Arán, Vicente J.
KeywordsMetabolite excretion
Leishmania
In vitro assay
Nitroindazole
Ultrastructural alteration
Cytotoxicity
Issue Date2015
PublisherElsevier
CitationActa Tropica 148: 170-178 (2015)
AbstractThe antiprotozoal activity of some indazole-derived amines (2, 3, 5-8) as well as that of some simple structurally related 3-alkoxy-1-alkyl-5-nitroindazoles (1, 4) against promastigote and amastigote forms of Leishmania infantum and Leishmania braziliensis is reported. In some cases, these compounds showed in vitro activities against the different morphological forms of Leishmania similar to or higher than those of the reference drug glucantime; this fact, along with low unspecific cytotoxicities against macrophages shown by some of them, led to good selectivity indexes (SI). The high efficiency of some 5-nitroindazoles against the mentioned protozoa was confirmed by further in vitro studies on infection rates. Complementary analyses by <sup>1</sup>H NMR of the changes on the metabolites excreted by parasites after treatment with the more active indazole derivatives in many cases showed the decreased excretion of succinate and increased levels of acetate, lactate and alanine, as well as, in some cases, the appearance of glycine and pyruvate as new metabolites. Damage caused by indazoles at the glycosomal or mitochondrial level are consistent with these metabolic changes as well as with the huge ultrastructural alterations observed by transmission electron microscopy (TEM), especially affecting the mitochondria and other cytoplasmic organelles.
URIhttp://hdl.handle.net/10261/117670
DOI10.1016/j.actatropica.2015.04.028
Identifiersdoi: 10.1016/j.actatropica.2015.04.028
issn: 0001-706X
e-issn: 1873-6254
Appears in Collections:(IQM) Artículos
Files in This Item:
File Description SizeFormat 
accesoRestringido.pdf15,38 kBAdobe PDFThumbnail
View/Open
Show full item record
 

Related articles:


WARNING: Items in Digital.CSIC are protected by copyright, with all rights reserved, unless otherwise indicated.