Trypanosoma cruzi: Inhibition of parasite growth and respiration by oxazolo(thiazolo)pyridine derivatives and its relationship to redox potential andlipophilicity

Citation
Jd. Maya et al., Trypanosoma cruzi: Inhibition of parasite growth and respiration by oxazolo(thiazolo)pyridine derivatives and its relationship to redox potential andlipophilicity, EXP PARASIT, 99(1), 2001, pp. 1-6
Citations number
17
Language
INGLESE
art.tipo
Article
Categorie Soggetti
Microbiology
Journal title
EXPERIMENTAL PARASITOLOGY
ISSN journal
0014-4894 → ACNP
Volume
99
Issue
1
Year of publication
2001
Pages
1 - 6
Database
ISI
SICI code
0014-4894(200109)99:1<1:TCIOPG>2.0.ZU;2-#
Abstract
Chagas' disease constitutes a therapeutic challenge because presently avail able drugs have wide toxicity to the host and are generally ineffective in the chronic stages of the disease. A series of oxazolo(thiazolo)pyridene de rivatives were studied on Trypanosoma cruzi epimastigote growth and oxygen consumption and their electrochemical (redox) potentials and lipophilicity. The derivatives produced different degrees of parasite growth and respirat ion inhibition on CL Brener, LQ, and Tulahuen strains of T. cruzi epimastig otes. Respiratory chain inhibition appears to be a determinant of the trypa nosomicidal activity of these compounds, since a significant correlation be tween respiration and culture growth inhibition was found. A similar correl ation was found, within the different structural subfamilies, between toxic effects and the ability of the compounds to be oxidized in aqueous media. The inhibition of respiration and of parasite growth in culture increases w ith the lipophilicity of the substituents on the oxazolopyridine nucleus. N o difference in the action of these derivatives was found among the differe nt parasite strains. It is concluded that these compounds may have a potent ial usefulness in the treatment of Chagas' disease. (C) 2001 Academic Press .