Activity of Megazol, a Trypanocidal Nitroimidazole, Is Associated with DNA Damage

Autor: Enanga, Bertin, Ariyanayagam, Mark R., Stewart, Mhairi L., Barrett, Michael P.
Zdroj: Antimicrobial Agents and Chemotherapy; October 2003, Vol. 47 Issue: 10 p3368-3370, 3p
Abstrakt: ABSTRACTDNA damage associated with the trypanocidal activity of megazol [2-amino-5-(1-methyl-5-nitro-2-imidazolyl)-1,3,4-thiadiazole] was shown in experiments in which DNA repair-deficient RAD51−/−Trypanosoma bruceimutants were found to be hypersensitive to the drug. Parasites resistant to megazol were selected and showed modest cross-resistance to other trypanocides, although neither drug efflux nor changes to intracellular thiols correlated with resistance.
Databáze: Supplemental Index