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  • Preparation and antileishmanial activity of lipophilic N-alkyl diamines.

Preparation and antileishmanial activity of lipophilic N-alkyl diamines.

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie (2008-02-12)
Cristiane F da Costa, Elaine S Coimbra, Fernanda G Braga, Roberta C N dos Reis, Adilson D da Silva, Mauro V de Almeida
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 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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
4-(Bromomethyl)pyridine hydrobromide, 97%