Synthesis and in vitro evaluation of potential antichagasic hydroxymethylnitrofurazone (NFOH-121): a new nitrofurazone prodrug |
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| Authors: | Chung Man-Chin Güido Rafael Victório Carvalho Martinelli Tatiane Favarato Gonçalves Marinei Ferreira Polli Michelle Carneiro Botelho Katia Cirlene Alves Varanda Eliana Aparecida Colli Walter Miranda M Terêsa M Ferreira Elizabeth Igne |
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| Affiliation: | Lapdesf- Laboratório de Pesquisa e Desenvolvimento de Fármacos, Departamento de Fármacos e Medicamentos, Faculdade de Ciências Farmacêuticas, UNESP, Araraquara, Caixa Postal 502, CEP 14.801-902, SP, Brazil. |
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| Abstract: | The synthesis of mutual prodrugs of nitrofurazone with primaquine, using specific and nonspecific spacer groups, has been previously attempted seeking selective antichagasic agents. The intermediate reaction product, hydroxymethylnitrofurazone (NFOH-121), was isolated and tested in LLC-MK(2) culture cells infected with trypomastigotes forms of Trypanosoma cruzi showing higher trypanocidal activity than nitrofurazone and benznidazol in all stages. The mutagenicity tests showed that the prodrug was less toxic than the parent drug. Degradation assays were carried out in pH 1.2 and 7.4. |
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