English   español  
Please use this identifier to cite or link to this item: http://hdl.handle.net/10261/83061
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

Antiprotozoal activity of 1-phenethyl-4-aminopiperidine derivatives

AuthorsDardonville, Christophe ; Fernández-Fernández, Cristina ; Gibbons, Sarah-Louise; Jagerovic, Nadine ; Nieto, Lidia ; Ryan, Gary; Kaiser, Marcel; Brun, Reto
Issue Date2009
PublisherAmerican Society for Microbiology
CitationAntimicrobial Agents and Chemotherapy 53: 3815- 3821 (2009)
AbstractA series of 44 4-aminopiperidine derivatives was screened in vitro against four protozoan parasites (Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, and Plasmodium falciparum). This screening identified 29 molecules selectively active against bloodstream-form T. b. rhodesiense trypomastigotes, with 50% inhibitory concentrations (IC50) ranging from 0.12 to 10 μM, and 33 compounds active against the chloroquine- and pyrimethamine-resistant K1 strain of P. falciparum (IC50 range, 0.17 to 5 μM). In addition, seven compounds displayed activity against intracellular T. cruzi amastigotes in the same range as the reference drug benznidazole (IC50, 1.97 μM) but were also cytotoxic to L-6 cells, showing little selectivity for T. cruzi. None of the molecules tested showed interesting antileishmanial activity against axenic amastigotes of L. donovani. To our knowledge, this is the first report of the antitrypanosomal activity of molecules bearing the 4-aminopiperidine skeleton.
Publisher version (URL)http://dx.doi.org/10.1128/AAC.00124-09
URIhttp://hdl.handle.net/10261/83061
DOI10.1128/AAC.00124-09
Identifiersdoi: 10.1128/AAC.00124-09
issn: 0066-4804
e-issn: 1098-6596
Appears in Collections:(IQM) Artículos
Files in This Item:
File Description SizeFormat 
Dardonville et al_AAC_2009_postprint.pdf236,07 kBAdobe PDFThumbnail
View/Open
Show full item record
Review this work
 

Related articles:


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