Synthesis and antileishmanial activity of lipophilic aromatic aminoalcohols

In this work, we report on the preparation and evaluation of the in vitro antileishmanial activity of a series of lipophilic aromatic aminoalcohols. All compounds were assessed for their in vitro antiproliferative activity against promastigotes of three Leishmania species. The most lipophilic aminoa...

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Bibliographic Details
Published in:TheScientificWorld 2010-01, Vol.10, p.1067-1072
Main Authors: Reis Corrales, Roberta Novaes, Pinheiro, Liliane Sena, Coimbra, Elaine Soares, Da Silva, Adilson David, Le Hyaric, Mireille
Format: Article
Language:English
Subjects:
Alcohols
Amino acids
Amino Alcohols - chemical synthesis
Amino Alcohols - pharmacology
Animals
Antiprotozoal Agents - chemical synthesis
Antiprotozoal Agents - pharmacology
Chemical properties
Chemical synthesis
Composition
Leishmania - drug effects
Leishmania - metabolism
Lipid Metabolism
Methods
Polyamines - metabolism
Production processes
Review
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Summary:In this work, we report on the preparation and evaluation of the in vitro antileishmanial activity of a series of lipophilic aromatic aminoalcohols. All compounds were assessed for their in vitro antiproliferative activity against promastigotes of three Leishmania species. The most lipophilic aminoalcohols bearing an aliphatic moiety with eight to 12 carbon atoms displayed a good activity against L. amazonensis and L. major, and two of them also showed antiproliferative activity against L. chagasi. The best results were obtained for the N-dodecanoyl ethylenediamine derivative and for N-decyl aminoalcohol (IC50=5.2 and 0.7 microM, respectively).
ISSN:1537-744X
2356-6140
1537-744X
DOI:10.1100/tsw.2010.106