Title:Biological Properties of Heterocyclic Pyridinylimines and Pyridinylhydrazones
Volume: 13
Issue: 1
Author(s): Francislene J. Martins, Rebeca Mol Lima, Juliana Alves dos Santos, Patricia de Almeida Machado, Elaine Soares Coimbra, Adilson David da Silva and Nádia Rezende Barbosa Raposo
Affiliation:
Keywords:
Heteroaromatic imines, heterocyclic Schiff bases, pyridinylimines, pyridinylhydrazones, antileishmanial activity,
antioxidant activity.
Abstract: This work describes the synthesis and biological properties of a series of 2- and 4-
pyridinylimines and pyridinylhydrazones. All compounds were evaluated in vitro against two species
of Leishmania. The antioxidant activity and the toxic effect against murine peritoneal macrophages of the compounds
were also performed. The synthesized compounds showed significant antileishmanial and antioxidant activities. For the
antileishmanial assay, compounds 1a, 1d and 2a were active against the Leishmania species, and compound 2a was the
most effective on promastigotes (IC50 value = 3.38 µM) and amastigotes (IC50 value = 18.96 µM) of L. amazonensis. Only
compound 2a exhibited toxicity against murine peritoneal macrophages (CC50 of 54.35 µM). However, this compound
was 2.8 times more destructive to the intracellular amastigotes than the host cell. Regarding the antioxidant activity, compounds
1a and 2a exhibited a strong antioxidant effect (IC50 values of 8.79 µM and 19.82 µM), compound 1a being better
than the L-ascorbic acid (9.48 µM), used as reference.
