Specific chemotherapy of Chagas disease: relevance, current limitations and new approaches

JA Urbina - Acta tropica, 2010 - Elsevier
A critical review of the development of specific chemotherapeutic approaches for the
management of American Trypanosomiasis or Chagas disease is presented, including …

Synthetic nitroimidazoles: biological activities and mutagenicity relationships

A Mital - Scientia pharmaceutica, 2009 - mdpi.com
Parasitic and bacterial infections affecting the gastrointestinal tract represent a significant
cause of morbidity and mortality worldwide. Nitroheterocyclic drugs have been available …

Design and synthesis of a series of melamine-based nitroheterocycles with activity against trypanosomatid parasites

A Baliani, GJ Bueno, ML Stewart… - Journal of medicinal …, 2005 - ACS Publications
The parasites that give rise to human African trypanosomiasis (HAT) are auxotrophs for
various nutrients from the human host, including purines. They have specialist nucleoside …

Trypanosoma cruzi: effect and mode of action of nitroimidazole and nitrofuran derivatives

JD Maya, S Bollo, LJ Nunez-Vergara, JA Squella… - Biochemical …, 2003 - Elsevier
With the aim of determining the actual target (s) of nitro-group bearing compounds
considered as possible leads for the development of drugs against Chagas' disease, we …

Uptake and mode of action of drugs used against sleeping sickness

H Denise, MP Barrett - Biochemical pharmacology, 2001 - Elsevier
Sleeping sickness is resurgent in Africa. Adverse side-effects and drug-resistance are
undermining the few drugs currently licensed for use against this disease, which is caused …

[HTML][HTML] Aspectos mecanísticos da bioatividade e toxicidade de nitrocompostos

FR Paulai, SHP Serrano, LC Tavares - Química Nova, 2009 - SciELO Brasil
Nitrocompounds are bioactive molecules used as antibacterial, antiparasitic and antitumoral
agents. In the past of years, these molecules have been broadly studied in several fields …

Trypanocidal activity of melamine-based nitroheterocycles

ML Stewart, GJ Bueno, A Baliani, B Klenke… - Antimicrobial agents …, 2004 - Am Soc Microbiol
ABSTRACT A series of nitroheterocyclic compounds were designed with linkages to
melamine or benzamidine groups that are known substrates of the P2 aminopurine and …

Cytotoxic and genotoxic effects of megazol, an anti-Chagas' disease drug, assessed by different short-term tests

P Poli, MA de Mello, A Buschini, RA Mortara… - Biochemical …, 2002 - Elsevier
Cyto-and genotoxicity induced by drugs can limit the dose and duration of treatment, can
adversely affect patient quality of life, and may be life-threatening. Two drugs are currently …

Megazol combined with suramin: a chemotherapy regimen which reversed the CNS pathology in a model of human African trypanosomiasis in mice

B Enanga, M Keita, G Chauviere… - Tropical Medicine & …, 1998 - Wiley Online Library
Chemotherapy for human African trypanosomiasis (HAT), or sleeping sickness, is unreliable
because of resistance, refraction and toxic and adverse side‐effects. Using a long‐term …

[HTML][HTML] Megazol and its bioisostere 4H-1,2,4-triazole: comparing the trypanocidal, cytotoxic and genotoxic activities and their in vitro and in silico interactions with the …

AS Carvalho, K Salomão, SL Castro… - Memórias do Instituto …, 2014 - SciELO Brasil
Megazol (7) is a 5-nitroimidazole that is highly active against Trypanosoma cruzi and
Trypanosoma brucei, as well as drug-resistant forms of trypanosomiasis. Compound 7 is not …