1,2,5-Oxadiazole N-oxide derivatives and related compounds as potential antitrypanosomal drugs: structure-activity relationships.

摘要: The syntheses of a new series derivatives 1,2,5-oxadiazole N-oxide, benzo[1,2-c]1,2,5-oxadiazole and quinoxaline di-N-oxide are described. In vitro antitrypanosomal activity these compounds was tested against epimastigote forms Trypanosoma cruzi. For the most effective drugs, IIIe IIIf, 50% inhibitory dose (ID50) determined as well their cytotoxicity mammalian fibroblasts. Electrochemical studies ESR spectroscopy show that highest activities observed associated with facile monoelectronation N-oxide moiety. Lipophilic−hydrophilic balance could also play an important role in effectiveness antichagasic drugs.