Authors
Man-Chin Chung, Rafael Victório Carvalho Güido, Tatiane Favarato Martinelli, Marinei Ferreira Gonçalves, Michelle Carneiro Polli, Katia Cirlene Alves Botelho, Eliana Aparecida Varanda, Walter Colli, M Terêsa M Miranda, Elizabeth Igne Ferreira
Publication date
2003/11/3
Journal
Bioorganic & medicinal chemistry
Volume
11
Issue
22
Pages
4779-4783
Publisher
Pergamon
Description
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.
Total citations
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