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Synthesis and Antitrypanosomal Profile of Novel Hydrazonoyl Derivatives

[ Vol. 16 , Issue. 4 ]

Author(s):

Natália N. Santiago, Giulianna P. de Alcântara, Juliana S. da Costa, Samir A. Carvalho, Juliana M.C. Barbosa, Kelly Salomão, Solange L. de Castro, Henrique M.G. Pereira and Edson F. da Silva*   Pages 487 - 494 ( 8 )

Abstract:


Background: Approximately, 5-7 million people are infected with T. cruzi in the world, and approximately 10,000 people per year die of complications linked to this disease.

Methods: This work describes the construction of a new family of hidrazonoyl substituted derivatives, structurally designed exploring the molecular hybridization between megazol and nitrofurazone.

Results and Discussion: The compounds were evaluated for their in vitro activity against bloodstream trypomastigotes of Trypanosoma cruzi, etiological agent of Chagas disease, and for their potential toxicity to mammalian cells.

Conclusion: Among these hydrazonoyl derivatives, we identified the derivative (4) that showed trypanocidal activity (IC50/24 h = 15.0 µM) similar to Bz, the standard drug, and low toxicity to mammalian cells, reaching an SI value of 18.7.

Keywords:

Hydrazonoyl, megazol, nitrofurazone, Chagas' disease, Trypanosoma cruzi, chemotherapy.

Affiliation:

Instituto de Tecnologia em Farmacos, Farmanguinhos, Laboratorio de sintese 1, Fundacao Oswaldo Cruz, Rio de Janeiro, RJ, Instituto de Tecnologia em Farmacos, Farmanguinhos, Laboratorio de sintese 1, Fundacao Oswaldo Cruz, Rio de Janeiro, RJ, Instituto de Tecnologia em Farmacos, Farmanguinhos, Laboratorio de sintese 1, Fundacao Oswaldo Cruz, Rio de Janeiro, RJ, Instituto de Tecnologia em Farmacos, Farmanguinhos, Laboratorio de sintese 1, Fundacao Oswaldo Cruz, Rio de Janeiro, RJ, Laboratorio de Biologia Celular, Instituto Oswaldo Cruz, Fundacao Oswaldo Cruz, Rio de Janeiro, RJ, Laboratorio de Biologia Celular, Instituto Oswaldo Cruz, Fundacao Oswaldo Cruz, Rio de Janeiro, RJ, Laboratorio de Biologia Celular, Instituto Oswaldo Cruz, Fundacao Oswaldo Cruz, Rio de Janeiro, RJ, Programa de Pos-Graduacao em Quimica, Instituto de Quimica, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Instituto de Tecnologia em Farmacos, Farmanguinhos, Laboratorio de sintese 1, Fundacao Oswaldo Cruz, Rio de Janeiro, RJ

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