Synthesis and in vitro Antitrypanosomal Activity of Novel Nifurtimox Analogues.

Abstract

2005 Medicinal chemistry V 1100 Synthesis and in vitro Antitrypanosomal Activity of Novel Nifurtimox Analogues. -The synthesis of novel analogues (I) of Nifurtimox, a 5-nitrofuran derivative, and their in vitro activity against Trypanosoma cruzi epimastigotes are described. (Ia) and (Ib) are the most potent compounds. The change of O by S, cf. (Ic), reduces the activity. -(POZAS, R.; CARBALLO, J.; CASTRO, C.; RUBIO*, J.; Bioorg. Med. Chem.

In vitro activity of thienyl-2-nitropropene compounds against Trypanosoma cruzi

“…and thereby inhibit its function (De Souza et al 2002) and (ii) the nitro group, which might produce oxidative stress by interacting with macromolecules through the production of nitrous derivatives (Henderson et al 1988, Stoppani 1999, Cerecetto et al 2000, Enanga et al 2003, De Oliveira et al 2003, Olea-Azar et al 2003, Stewart et al 2004, Pozas et al 2005, Quesada et al 2006). …”

“…Several imidazole and nitrofuran analogues have been tested against T. cruzi and these analogues have been found to exert similar activities against the epimastigote and the trypomastigote forms (Pozas et al 2005). Although megazol, a 5-nitroimidazole derivative, has been used to treat Trypanosoma brucei infection (Darsaud et al 2004) and at least one study highlights its therapeutic efficacy against T. cruzi infection , its utility has been called into question as a result of reports that it can cause chromosomal alterations and DNA damage (Enanga et al 2003, Nesslany et al 2004.…”

New Treatments for Chagas Disease and the Relationship between Chagasic Patients and Cancers

“…During the chronic phase it is common for adults to develop cardiac and/or digestive problems, leading to 400 thousands deaths per year in Latin America [6]. Furthermore, endemic countries suffer with high medical costs and social loses due to the existing comorbidities and inabilities generated by the disease.…”