Biomedicine & Pharmacotherapy 2009-01-01

Preparation and antileishmanial activity of lipophilicN-alkyl diamines

Cristiane F. da Costa, Elaine S. Coimbra, Fernanda G. Braga, Roberta C.N. dos Reis, Adilson D. da Silva, Mauro V. de Almeida, Cristiane F. da Costa, Elaine S. Coimbra, Fernanda G. Braga, Roberta C.N. dos Reis, Adilson D. da Silva, Mauro V. de Almeida, Cristiane F. da Costa, Elaine S. Coimbra, Fernanda G. Braga, Roberta C.N. dos Reis, Adilson D. da Silva, Mauro V. de Almeida

Index: Biomed. Pharmacother. 63(1) , 40-2, (2009)

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Abstract

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 μM. 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.