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