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Indazole N-oxide derivatives as antiprotozoal agents: Synthesis, biological evaluation and mechanism of action studies

AuthorsGerpe, Alejandra; Aguirre, Gabriela; Boiani, Lucía; Cerecetto, Hugo; González, Mercedes; Olea-Azar, Claudio; Rigol, C.; Maya, Juan D.; Morello, A.; Piro, Óscar E.; Arán, Vicente J. ; Azqueta, Amaya; Ceráin, A. L. de; Monge, M. Ángeles ; Yaluff, G.
Issue Date2006
PublisherPergamon Press
CitationBioorganic and Medicinal Chemistry 14: 3467- 3480 (2006)
AbstractA series of indazole N-oxide derivatives have been synthesized and their antichagasic and leishmanocidal properties studied. 3-Cyano-2-(4-iodophenyl)-2H-indazole N1-oxide exhibited interesting antichagasic activity on the two parasitic strains and the two parasitic stages evaluated. Furthermore, besides its trypanocidal activity, 3-cyano-2-(4-nitrophenyl)-2H-indazole N1-oxide showed leishmanocidal activity in the three parasitic strains evaluated. To gain insight into the mechanism of action, electrochemical behaviour, ESR experiment, inhibition of parasitic respiration and QSAR were performed. © 2006.
Identifiersdoi: 10.1016/j.bmc.2006.01.007
issn: 0968-0896
e-issn: 1464-3391
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