Published in

American Society for Microbiology, Antimicrobial Agents and Chemotherapy, 9(53), p. 3815-3821, 2009

DOI: 10.1128/aac.00124-09

Links

Tools

Export citation

Search in Google Scholar

Antiprotozoal activity of 1-phenethyl-4-aminopiperidine derivatives

Journal article published in 2009 by Christophe Dardonville, Fernandez-Fernandez C., Cristina Fernandez-Fernandez, Sarah-Louise Gibbons, Nadine Jagerovic ORCID, Lidia Nieto, Gary Ryan, Marcel Kaiser, Reto Brun
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

Full text: Download

Green circle
Preprint: archiving allowed
Upload
Green circle
Postprint: archiving allowed
Upload
Orange circle
Published version: archiving restricted
Upload
Policy details
Data provided by SHERPA/RoMEO

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 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. Copyright © 2009, American Society for Microbiology. All Rights Reserved.