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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Synthesis and in vitro evaluation of potential antichagasic hydroxymethyinitrofurazone (NFOH-121): A new nitrofurazone prodrug

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Author(s):
Chung, Man-Chin ; Guido, 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. [9] ; Ferreira, Elizabeth Igne
Total Authors: 10
Document type: Journal article
Source: Bioorganic & Medicinal Chemistry; v. 11, n. 22, p. 4779-4783, Nov. 2003.
Field of knowledge: Biological Sciences - Biochemistry
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. (AU)

FAPESP's process: 95/04562-3 - Studies on Specific Ligands and Enzymes from Trypanosoma cruzi
Grantee:Walter Colli
Support type: Research Projects - Thematic Grants
FAPESP's process: 01/01192-3 - Potential antitripanosomal derived from nitro-heterocyclic compounds
Grantee:Elizabeth Igne Ferreira
Support type: Research Projects - Thematic Grants