Gerpe Alejandra, Aguirre Gabriela, Boiani Lucía, Cerecetto Hugo, González Mercedes, Olea-Azar Claudio, Rigol Carolina, Maya Juan D, Morello Antonio, Piro Oscar E, Arán Vicente J, Azqueta Amaia, de Ceráin Adela López, Monge Antonio, Rojas María Antonieta, Yaluff Gloria
Departamento de Química Orgánica, Facultad de Química-Facultad de Ciencias, Universidad de la República, Iguá 4225, Montevideo 11400, Uruguay.
Bioorg Med Chem. 2006 May 15;14(10):3467-80. doi: 10.1016/j.bmc.2006.01.007. Epub 2006 Feb 17.
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.
已合成了一系列吲唑 N-氧化物衍生物，并研究了它们的抗恰加斯病和杀利什曼原虫特性。3-氰基-2-(4-碘苯基)-2H-吲唑 N1-氧化物在评估的两种寄生虫菌株和两个寄生虫阶段表现出有趣的抗恰加斯病活性。此外，除了其杀锥虫活性外，3-氰基-2-(4-硝基苯基)-2H-吲唑 N1-氧化物在评估的三种寄生虫菌株中显示出杀利什曼原虫活性。为深入了解其作用机制，进行了电化学行为、电子自旋共振实验、寄生虫呼吸抑制和定量构效关系研究。
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