1,2,5-Oxadiazole N-oxide derivatives and related compounds as potential antitrypanosomal drugs: structure-activity relationships.Show others and affiliations
1999 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 42, no 11, p. 1941-50Article in journal (Refereed) Published
Abstract [en]
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 activity of these compounds was tested against epimastigote forms of Trypanosoma cruzi. For the most effective drugs, derivatives IIIe and IIIf, the 50% inhibitory dose (ID50) was determined as well as their cytotoxicity against mammalian fibroblasts. Electrochemical studies and ESR spectroscopy show that the highest activities observed are associated with the facile monoelectronation of the N-oxide moiety. Lipophilic-hydrophilic balance of the compounds could also play an important role in their effectiveness as antichagasic drugs.
Place, publisher, year, edition, pages
American Chemical Society (ACS), 1999. Vol. 42, no 11, p. 1941-50
National Category
Medicinal Chemistry
Identifiers
URN: urn:nbn:se:kau:diva-80288DOI: 10.1021/jm9805790ISI: 000080736800009PubMedID: 10354402OAI: oai:DiVA.org:kau-80288DiVA, id: diva2:1468429
2020-09-172020-09-172020-09-29Bibliographically approved