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 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).
Reis Corrales
Roberta Novaes
RN
Departamento de Química, I.C.E., Universidade Federal de Juiz de Fora, Campus Universitário, Juiz de Fora, Minas Gerais, Brazil. robertacnr@bol.com.br
Pinheiro
Liliane Sena
LS
Coimbra
Elaine Soares
ES
Da Silva
Adilson David
AD
Le Hyaric
Mireille
M
D000605:Amino Alcohols / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D007891:Leishmania / Q000187:drug effects* / Q000378:metabolism; D050356:Lipid Metabolism; D011073:Polyamines / Q000378:metabolism
D000605:Amino Alcohols; D000981:Antiprotozoal Agents; D011073:Polyamines