2. Academic Validation
  3. Synthesis and tripanocidal activity of ferrocenyl and benzyl diamines against Trypanosoma brucei and Trypanosoma cruzi

Synthesis and tripanocidal activity of ferrocenyl and benzyl diamines against Trypanosoma brucei and Trypanosoma cruzi

  • Bioorg Med Chem Lett. 2014 Apr 1;24(7):1707-10. doi: 10.1016/j.bmcl.2014.02.046.
Angela Maria Arenas Velásquez 1,  Acácio Ivo Francisco 2,  Andréa Akiko Nakaima Kohatsu 3,  Flavia Alves de Jesus Silva 3,  Danilo Fernando Rodrigues 4,  Rafaela Gomes da Silva Teixeira 2,  Bruna Galdorfini Chiari 5,  Maria Gabriela José de Almeida 5,  Vera Lucia Borges Isaac 5,  Maria D Vargas 2,  Regina Maria Barretto Cicarelli 6
Affiliations

Affiliations

  • 1 Departamento de Ciências Biológicas, Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista 'Júlio de Mesquita Filho', Rodovia Araraquara-Jaú Km 01-Campus, Araraquara 14.801-902, Brazil; Instituto de Química, Universidade Estadual Paulista 'Júlio de Mesquita Filho', Rua Prof. Francisco Degni, 55, Araraquara 14.800-900, Brazil. Electronic address: avellangel@gmail.com.
  • 2 Instituto de Química, Universidade Federal Fluminense, Campus do Valonguinho-Centro, Niterói 24.020-150, Brazil.
  • 3 Departamento de Ciências Biológicas, Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista 'Júlio de Mesquita Filho', Rodovia Araraquara-Jaú Km 01-Campus, Araraquara 14.801-902, Brazil.
  • 4 Departamento de Ciências Biológicas, Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista 'Júlio de Mesquita Filho', Rodovia Araraquara-Jaú Km 01-Campus, Araraquara 14.801-902, Brazil; Instituto de Química, Universidade Estadual Paulista 'Júlio de Mesquita Filho', Rua Prof. Francisco Degni, 55, Araraquara 14.800-900, Brazil.
  • 5 Departamento de Fármacos e Medicamentos, Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista 'Júlio de Mesquita Filho', Rodovia Araraquara-Jaú Km 01-Campus, Araraquara 14.801-902, Brazil.
  • 6 Departamento de Ciências Biológicas, Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista 'Júlio de Mesquita Filho', Rodovia Araraquara-Jaú Km 01-Campus, Araraquara 14.801-902, Brazil. Electronic address: reginacicarelli@gmail.com.
PMID: 24630563 DOI: 10.1016/j.bmcl.2014.02.046
Abstract

Trypanosoma brucei and Trypanosoma cruzi are the etiologic agents of sleeping sickness and Chagas disease, respectively, two of the 17 preventable tropical infectious diseases (NTD) which have been neglected by governments and organizations working in the health sector, as well as pharmaceutical industries. High toxicity and resistance are problems of the conventional drugs employed against trypanosomiasis, hence the need for the development of new drugs with trypanocidal activity. In this work we have evaluated the trypanocidal activity of a series of N1,N2-dibenzylethane-1,2-diamine hydrochlorides (benzyl diamines) and N1-benzyl,N2-methyferrocenylethane-1,2-diamine hydrochlorides (ferrocenyl diamines) against T. brucei and T. cruzi Parasite strains. We show that incorporation of the ferrocenyl group into the benzyl diamines increases the trypanocidal activity. The molecules exhibit potential trypanocidal activity in vitro against all Parasite strains. Cytotoxicity assay was also carried out to evaluate the toxicity in HepG2 cells.

Keywords

Benzyl diamines; Chagas disease; Ferrocenyl diamines; Sleeping sickness.

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