RESUMO
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.
Assuntos
Antiprotozoários/síntese química , Antiprotozoários/farmacologia , Diaminas/química , Diaminas/farmacologia , Leishmania/efeitos dos fármacos , Animais , Estrutura MolecularRESUMO
A number of lipophilic N-acyl-diamines and aldonamides have been synthesized and tested for their in vitro antiproliferative activity against Leishmania amazonensis and L. chagasi. Ribonamides, having one amino group, displayed good to moderate inhibition of parasite growth. The best result was obtained for compounds 10 and 15 with IC50 against L. chagasi below 5 microM.
