Preparation and antileishmanial activity of lipophilic N-alkyl diamines.
We report in this work the preparation and the in vitro antileishmanial activity of a series of long chains N-monoalkylated diamines and two pyridinediamine derivatives. Several compounds, tested for their in vitro antiproliferative activity against Leishmania amazonensis and Leishmania chagasi, displayed a good inhibition of parasite growth, with IC(50) below 10 microM. Compounds 10 (N-dodecyl-1,2-ethanediamine), 15 (N-decyl-1,3-propanediamine) and 20 (N-dodecyl-1,4-butanediamine) were 7.3, 2.6 and 3.6 times, respectively, more active than the reference drug amphotericin B against L. chagasi promastigote forms.
da Costa
Cristiane F
CF
Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Cidade Universitária, Campos Martelos, Juiz de Fora, MG, Brazil.
Coimbra
Elaine S
ES
Braga
Fernanda G
FG
dos Reis
Roberta C N
RC
da Silva
Adilson D
AD
de Almeida
Mauro V
MV
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D003959:Diamines / Q000737:chemistry* / Q000494:pharmacology*; D007891:Leishmania / Q000187:drug effects*; D015394:Molecular Structure
D000981:Antiprotozoal Agents; D003959:Diamines