Literature DB >> 14556793

Synthesis and in vitro evaluation of potential antichagasic hydroxymethylnitrofurazone (NFOH-121): a new nitrofurazone prodrug.

Man-Chin Chung1, 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.   

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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Year:  2003        PMID: 14556793     DOI: 10.1016/j.bmc.2003.07.004

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  15 in total

1.  Design and exploratory data analysis of a second generation of dendrimer prodrugs potentially antichagasic and leishmanicide.

Authors:  Jeanine Giarolla; Kerly Fernanda Mesquita Pasqualoto; Elizabeth I Ferreira
Journal:  Mol Divers       Date:  2013-08-29       Impact factor: 2.943

2.  Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.

Authors:  Juan C Engel; Kenny K H Ang; Steven Chen; Michelle R Arkin; James H McKerrow; Patricia S Doyle
Journal:  Antimicrob Agents Chemother       Date:  2010-06-14       Impact factor: 5.191

3.  Molecular modeling study on the disassembly of dendrimers designed as potential antichagasic and antileishmanial prodrugs.

Authors:  Jeanine Giarolla; Kerly F M Pasqualoto; Daniela G Rando; Márcio H Zaim; Elizabeth I Ferreira
Journal:  J Mol Model       Date:  2011-10-02       Impact factor: 1.810

4.  Hydroxymethylnitrofurazone:dimethyl-beta-cyclodextrin inclusion complex: a physical-chemistry characterization.

Authors:  Renato Grillo; Nathalie Ferreira Silva Melo; Carolina Morales Moraes; André Henrique Rosa; José Arnaldo Frutuoso Roveda; Carla M S Menezes; Elizabeth Igne Ferreira; Leonardo Fernandes Fraceto
Journal:  J Biol Phys       Date:  2008-02-27       Impact factor: 1.365

5.  Hydroxymethylnitrofurazone is active in a murine model of Chagas' disease.

Authors:  Carolina Davies; Rubén Marino Cardozo; Olga Sánchez Negrette; María Celia Mora; Man Chin Chung; Miguel Angel Basombrío
Journal:  Antimicrob Agents Chemother       Date:  2010-06-21       Impact factor: 5.191

6.  Hydroxymethylnitrofurazone treatment in indeterminate form of chronic Chagas disease: Reduced intensity of tissue parasitism and inflammation-A histopathological study.

Authors:  Cauê B Scarim; Cleverton R de Andrade; João A da Rosa; Jean L Dos Santos; Chung M Chin
Journal:  Int J Exp Pathol       Date:  2018-10-15       Impact factor: 1.925

7.  Genotoxicity revaluation of three commercial nitroheterocyclic drugs: nifurtimox, benznidazole, and metronidazole.

Authors:  Annamaria Buschini; Lisa Ferrarini; Susanna Franzoni; Serena Galati; Mirca Lazzaretti; Francesca Mussi; Cristina Northfleet de Albuquerque; Tânia Maria Araújo Domingues Zucchi; Paola Poli
Journal:  J Parasitol Res       Date:  2009-10-21

8.  Pharmacokinetics of hydroxymethylnitrofurazone, a promising new prodrug for Chagas' disease treatment.

Authors:  Eliana Ometto Pavan Serafim; Antonio Távora de Albuquerque E Silva; Andréia de Haro Moreno; Ednir de Oliveira Vizioli; Elizabeth Igne Ferreira; Rosângela Gonçalves Peccinini; Maria Lucia Ribeiro; Man Chin Chung
Journal:  Antimicrob Agents Chemother       Date:  2013-09-30       Impact factor: 5.191

9.  Hepatotoxicity in mice of a novel anti-parasite drug candidate hydroxymethylnitrofurazone: a comparison with Benznidazole.

Authors:  Carolina Davies; Nilay Dey; Olga Sanchez Negrette; Luis Antonio Parada; Miguel A Basombrio; Nisha Jain Garg
Journal:  PLoS Negl Trop Dis       Date:  2014-10-16

Review 10.  Synthetic Medicinal Chemistry in Chagas' Disease: Compounds at The Final Stage of "Hit-To-Lead" Phase.

Authors:  Hugo Cerecetto; Mercedes González
Journal:  Pharmaceuticals (Basel)       Date:  2010-03-25
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