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Indazole N-oxide derivatives as antiprotozoal agents: synthesis, biological evaluation and mechanism of action studies. 2006
Alejandra Gerpe, and
Gabriela Aguirre, and
Lucía Boiani, and
Hugo Cerecetto, and
Mercedes González, and
Claudio Olea-Azar, and
Carolina Rigol, and
Juan D Maya, and
Antonio Morello, and
Oscar E Piro, and
Vicente J Arán, and
Amaia Azqueta, and
Adela López de Ceráin, and
Antonio Monge, and
María Antonieta Rojas, and
Gloria Yaluff
Departamento de Química Orgánica, Facultad de Química-Facultad de Ciencias, Universidad de la República, Iguá 4225, Montevideo 11400, Uruguay.
A 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.
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