Activity of megazol, a trypanocidal nitroimidazole, is associated with DNA damage.
DNA 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 brucei mutants 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.
D000818:Animals; D004249:DNA Damage; D004268:DNA-Binding Proteins / Q000235:genetics; D018432:Drug Resistance, Multiple / Q000187:drug effects / Q000235:genetics; D020128:Inhibitory Concentration 50; D009154:Mutation; D013830:Thiadiazoles / Q000737:chemistry / Q000494:pharmacology*; D014344:Trypanocidal Agents / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects / Q000235:genetics
D004268:DNA-Binding Proteins; D013830:Thiadiazoles; D014344:Trypanocidal Agents; C013378:megazol