Indazole N-oxide derivatives as antiprotozoal agents: Synthesis, biological evaluation and mechanism of action studies
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2006-05-15Metadata
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Gerpe, Alejandra
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Indazole N-oxide derivatives as antiprotozoal agents: Synthesis, biological evaluation and mechanism of action studies
Author
- Gerpe, Alejandra;
- Aguirre, Gabriela;
- Boiani, Lucía;
- Cerecetto, Hugo;
- González, Mercedes;
- Olea Azar, Claudio;
- Rigol Olsen, Carolina;
- Maya Arango, Juan;
- Morello Casté, Antonio;
- Piro, Oscar E.;
- Arán, Vicente J.;
- Azqueta, Amaia;
- López de Ceráin, Adela;
- Monge, Antonio;
- Rojas, María Antonieta;
- Yaluff, Gloria;
Abstract
A series of indazole N-oxide derivatives have been synthesized and their antichagasic and leishmanocidal properties studied. 3-Cyano-2-(4-iodophenyl)-2H-indazole N-1-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 N-1-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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BIOORGANIC & MEDICINAL CHEMISTRY Volume: 14 Issue: 10 Pages: 3467-3480 Published: MAY 15 2006
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