| Title | Antiprotozoal activity of 1-phenethyl-4-aminopiperidine derivatives. | | Author(s) | Dardonville C, Fernandez-Fernandez C, Gibbons SL, Jagerovic N, Nieto L, Ryan G, Kaiser M, Brun R | | Institution | Instituto de Química Médica, CSIC, Juan de la Cierva 3, E-28006 Madrid, Spain; Swiss Tropical Institute, Socinstrasse, 57, CH-4002 Basel, Switzerland. | | Source | Antimicrob Agents Chemother 2009 Jun 29. | | Abstract | A series of forty four 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 IC50 values ranging from 0.12 to 10 microM, and 33 compounds active against the chloroquine/pyrimethamine resistant K1 strain of P. falciparum in the 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 L6-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. | | Language | ENG | | Pub Type(s) | JOURNAL ARTICLE
| | PubMed ID | 19564359 |
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