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Title: Indazole N-oxide derivatives as antiprotozoal agents: synthesis, biological evaluation and mechanism of action studies. Author: Gerpe A, Aguirre G, Boiani L, Cerecetto H, González M, Olea-Azar C, Rigol C, Maya JD, Morello A, Piro OE, Arán VJ, Azqueta A, de Ceráin AL, Monge A, Rojas MA, Yaluff G. Journal: Bioorg Med Chem; 2006 May 15; 14(10):3467-80. PubMed ID: 16483783. 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 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.[Abstract] [Full Text] [Related] [New Search]