4.7 Article

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

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BIOORGANIC & MEDICINAL CHEMISTRY
卷 14, 期 10, 页码 3467-3480

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2006.01.007

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antichagasic activity; leishmanocidal activity; indazole N-oxide

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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. (c) 2006 Published by Elsevier Ltd.

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