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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Biological Properties of Heterocyclic Pyridinylimines and Pyridinylhydrazones

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

Volume 13 , Issue 1 , 2016

Page: [107 - 114] Pages: 8

DOI: 10.2174/1570180812666141216205601

Price: $65


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.

Keywords: Heteroaromatic imines, heterocyclic Schiff bases, pyridinylimines, pyridinylhydrazones, antileishmanial activity, antioxidant activity.

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