Author/Authors :
Man-Chin Chung، نويسنده , , Rafael Vict?rio Carvalho Güido، نويسنده , , Tatiane Favarato Martinelli، نويسنده , , Marinei Ferreira Gonçalves، نويسنده , , Michelle Carneiro Polli، نويسنده , , Katia Cirlene Alves Botelho، نويسنده , , Eliana Aparecida Varanda، نويسنده , , Walter Colli، نويسنده , , M. Terêsa M. Miranda، نويسنده , , Elizabeth Igne Ferreira، نويسنده ,
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-MK2 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.
