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Antiprotozoal activity of 1-phenethyl-4-aminopiperidine derivatives
JournalArticle (Originalarbeit in einer wissenschaftlichen Zeitschrift)
 
ID 533216
Author(s) Dardonville, Christophe; Fernández-Fernández, Cristina; Gibbons, Sarah-Louise; Jagerovic, Nadine; Nieto, Lidia; Ryan, Gary; Kaiser, Marcel; Brun, Reto
Author(s) at UniBasel Brun, Reto
Kaiser, Marcel
Year 2009
Title Antiprotozoal activity of 1-phenethyl-4-aminopiperidine derivatives
Journal Antimicrobial agents and chemotherapy : AAC
Volume 53
Number 9
Pages / Article-Number 3815-21
Abstract A 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 microM, and 33 compounds active against the chloroquine- and pyrimethamine-resistant K1 strain of P. falciparum (IC50 range, 0.17 to 5 microM). In addition, seven compounds displayed activity against intracellular T. cruzi amastigotes in the same range as the reference drug benznidazole (IC50, 1.97 microM) 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 American Society for Microbiology
ISSN/ISBN 0066-4804
edoc-URL http://edoc.unibas.ch/dok/A5843144
Full Text on edoc No
Digital Object Identifier DOI 10.1128/AAC.00124-09
PubMed ID http://www.ncbi.nlm.nih.gov/pubmed/19564359
ISI-Number WOS:000270014200027
Document type (ISI) Journal Article
 
   

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29/03/2024