Journal ArticleDOI
Trypanosoma cruzi: effect and mode of action of nitroimidazole and nitrofuran derivatives.
Juan Diego Maya,Soledad Bollo,Luis J. Núñez-Vergara,Juan A. Squella,Yolanda Repetto,Antonio Morello,Jacques Périé,G. Chauviere +7 more
Reads0
Chats0
TLDR
The results indicate that nifurtimox and related compounds act as redox cyclers, whereas the most active in the series, the 5-nitroimidazole megazol essentially acts as thiol scavenger particularly for trypanothione, the cofactor for try panothione reductase, an essential enzyme in the detoxification process.About:
This article is published in Biochemical Pharmacology.The article was published on 2003-03-15. It has received 155 citations till now. The article focuses on the topics: Trypanothione & Megazol.read more
Citations
More filters
Journal ArticleDOI
1,3,4-Thiadiazole: Synthesis, Reactions, and Applications in Medicinal, Agricultural, and Materials Chemistry
Journal ArticleDOI
Mode of action of natural and synthetic drugs against Trypanosoma cruzi and their interaction with the mammalian host.
Juan Diego Maya,Bruce K. Cassels,Patricio Iturriaga-Vásquez,Jorge Ferreira,Mario Faundez,Norbel Galanti,Arturo Ferreira,Antonio Morello +7 more
TL;DR: A large set of chemicals of plant origin and a few animal metabolites active against T. cruzi are enumerated and their likely modes of action are briefly discussed.
Journal ArticleDOI
Drugs and drug resistance in African trypanosomiasis.
V. Delespaux,Harry P. de Koning +1 more
TL;DR: The use of current drugs against human and veterinary African trypanosomiasis, the prevalence, causes and mechanisms of drug resistance and new developments in trypanOSomiasis therapy such as the introduction of nifurtimox and DB289 are discussed.
Journal ArticleDOI
Dithiol proteins as guardians of the intracellular redox milieu in parasites: old and new drug targets in trypanosomes and malaria-causing plasmodia.
TL;DR: Inhibitors of antioxidant enzymes such as trypanothione reductase are, indeed, parasiticidal but they can also delay or prevent resistance against a number of other antiparasitic drugs.
Journal ArticleDOI
Activation of Benznidazole by Trypanosomal Type I Nitroreductases Results in Glyoxal Formation
TL;DR: These experiments indicate that the reduction of benznidazole by type I nitroreductase activity leads to the formation of highly reactive metabolites and that the expression of this enzyme is key to the trypanocidal properties displayed by the prodrug.
References
More filters
Journal ArticleDOI
A critical review on Chagas disease chemotherapy.
TL;DR: A historical introduction of drugs assayed against Chagas disease beginning in 1912 with the works of Mayer and Rocha Lima up to the experimental use of nitrofurazone, and a survey about new classes of synthetic and natural compounds studied after 1992/1993.
Journal ArticleDOI
Susceptibility and natural resistance of Trypanosoma cruzi strains to drugs used clinically in Chagas disease.
TL;DR: Most of the 47 studied strains were either sensitive or resistant to both compounds, an intriguing finding considering that nifurtimox and benznidazole apparently have different mechanisms of action against T. cruzi.
Journal ArticleDOI
In vivo effects of difluoromethylornithine on trypanothione and polyamine levels in bloodstream forms of Trypanosoma brucei.
TL;DR: Depletion of this metabolite may be an important contributory factor to the selective toxic effect of DFMO, particularly in its synergistic effect with other trypanocidal drugs.
Journal ArticleDOI
Enzymatic reduction studies of nitroheterocycles
Cécile Viodé,Nadir Bettache,Narimantas Cenas,R. Luise Krauth-Siegel,G. Chauviere,Norbert Bakalara,Jacques Périé +6 more
TL;DR: As shown here, Megazol interferes with the oxygen metabolism of the parasite, but its extra activity when compared to Nifurtimox may be related to other features not yet identified.
Journal ArticleDOI
Identification of a novel, thiol-containing co-factor essential for glutathione reductase enzyme activity in trypanosomatids.
Alan H. Fairlamb,Anthony Cerami +1 more
TL;DR: Evidence is presented showing that co-factor contains enzymatically reducible thiol group(s), essential for activity, and possibly unique to the Kinetoplastida.