Synthesis, Cytotoxicity and Antileishmanial Activity of Aza-stilbene derivatives

Authors

  • Daniela T. S. de Paula Departamento de Parasitologia, Microbiologia e Imunologia, I.C.B., Universidade Federal de Juiz de Fora, Cidade Universitária, Juiz de Fora, MG, 36036-900, Brazil;
  • Gustavo S. G. de Carvalho Departamento de Química, I.C.E., Universidade Federal de Juiz de Fora, Cidade Universitária, Juiz de Fora, MG, 36036-900, Brazil.
  • Ayla C. Almeida Departamento de Parasitologia, Microbiologia e Imunologia, I.C.B., Universidade Federal de Juiz de Fora, Cidade Universitária, Juiz de Fora, MG, 36036-900, Brazil;
  • Mariana Lourenco Departamento de Parasitologia, Microbiologia e Imunologia, I.C.B., Universidade Federal de Juiz de Fora, Cidade Universitária, Juiz de Fora, MG, 36036-900, Brazil;
  • Adilson D. da Silva Departamento de Química, I.C.E., Universidade Federal de Juiz de Fora, Cidade Universitária, Juiz de Fora, MG, 36036-900, Brazil.
  • Elaine S. Coimbra Departamento de Parasitologia, Microbiologia e Imunologia, I.C.B., Universidade Federal de Juiz de Fora, Cidade Universitária, Juiz de Fora, MG, 36036-900, Brazil;

DOI:

https://doi.org/10.13171/mjc.2.3.2013.07.02.16

Abstract

Stilbenes are compounds found in numerous medicinal plants and food products with some known biological and even antileishmanial activity. This paper describes the preparation of Aza-stilbene derivatives and their in vitro biological activities against Leishmania species. Most of the compounds with hydroxyl groups (2a, 2b, 2d, 2e and 2f) showed interesting results against three Leishmania species tested. Compound 2f showed the best activity against intracellular forms of L. amazonensis, with IC50 of 7.48 μM, very similar when compared to reference drug Miltefosine. It not possible associate NO production with leishmanicidal activity for all aza-stilbene derivatives. It is noteworthy that none of compounds tested showed cytotoxicity against macrophages.

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Published

2013-02-07

Issue

Vol. 2 No. 3 (2013)

Section

Medicinal Chemistry

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