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Design, synthesis and antitrypanosomal activity of some nitrofurazone 1,2,4-triazolic bioisosteric analogues.
Silva, Fredson T; Franco, Caio H; Favaro, Denize C; Freitas-Junior, Lucio H; Moraes, Carolina B; Ferreira, Elizabeth I.
Afiliação
  • Silva FT; School of Pharmaceutical Sciences, University of São Paulo, Avenida Prof. Lineu Prestes, 580, Bl. 13, São Paulo, São Paulo, Brazil.
  • Franco CH; National Laboratory of Biosciences, National Center for Research on Energy and Materials, Rua Giuseppe Máximo Scolfaro, 10000, Campinas, São Paulo, Brazil.
  • Favaro DC; Institute of Chemistry, University of São Paulo, Avenida Prof. Lineu Prestes, 748, São Paulo, São Paulo, Brazil; Department of Chemistry, Institute of Exact Sciences, Federal University of Minas Gerais, Belo Horizonte, Brazil.
  • Freitas-Junior LH; National Laboratory of Biosciences, National Center for Research on Energy and Materials, Rua Giuseppe Máximo Scolfaro, 10000, Campinas, São Paulo, Brazil.
  • Moraes CB; National Laboratory of Biosciences, National Center for Research on Energy and Materials, Rua Giuseppe Máximo Scolfaro, 10000, Campinas, São Paulo, Brazil.
  • Ferreira EI; School of Pharmaceutical Sciences, University of São Paulo, Avenida Prof. Lineu Prestes, 580, Bl. 13, São Paulo, São Paulo, Brazil. Electronic address: hajudan@usp.br.
Eur J Med Chem ; 121: 553-560, 2016 Oct 04.
Article em En | MEDLINE | ID: mdl-27318979
Chagas disease, caused by Trypanosoma cruzi, is a parasitosis that predominates in Latin America. It is estimated that 25 million people are under the risk of infection and, in 2008, more than 10 thousand deaths were registered. The only two drugs available in the therapeutics, nifurtimox and benznidazole, showed to be more effective in the acute phase of the disease. However, there is no standard treatment protocol effective for the chronic phase. Nitrofurazone (NF), an antimicrobial drug, has activity against T. cruzi, although being toxic. Considering the need for new antichagasic drugs, the existence of promising new therapeutic targets, as 14α-sterol demethylase and cruzain, and employing the bioisosterism and molecular hybridization approaches, four novel compounds were synthesized, characterized by melting point range, elemental analysis, IR and NMR spectroscopy. The compounds were tested against T. cruzi amastigotes in infected U2OS cells. All compounds showed selectivity towards T. cruzi and showed trypanomicidal activity in low micromolar range. The compound 3 showed potency similar to benznidazole, but lower efficacy. These results highlight the importance of the 1,2,4-triazole, thiosemicarbazonic and nitro group moieties for designing new efficient compounds, potentially for the chronic phase of Chagas disease.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Triazóis / Tripanossomicidas / Trypanosoma cruzi / Nitrofurazona Tipo de estudo: Guideline Limite: Humans Idioma: En Revista: Eur J Med Chem Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Brasil País de publicação: França
Texto completo
Adicionar na Minha BVS
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XML
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Triazóis / Tripanossomicidas / Trypanosoma cruzi / Nitrofurazona Tipo de estudo: Guideline Limite: Humans Idioma: En Revista: Eur J Med Chem Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Brasil País de publicação: França