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

被引:92
|
作者
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
机构
[1] Univ Republica, Dept Quim Organ, Fac Quim, Fac Ciencias, Montevideo 11400, Uruguay
[2] Univ Chile, Dept Quim Inorgan & Analit, Fac Ciencias Quim & farmaceut, Santiago 233, Chile
[3] Univ Chile, Fac Med, Dept Farmacol Clin Mol, Santiago 7, Chile
[4] Natl Univ La Plata, Dept Fis, Fac Ciencias Exactas, CONICET,IFLP, RA-1900 La Plata, Argentina
[5] CSIC, Inst Quim Med, E-28006 Madrid, Spain
[6] Univ Navarra, Ctr Invest Farmacobiol Aplicada, Navarra 31080, Spain
[7] Univ Nacl Asuncion, Inst Invest Ciencias Salud, Dept Trop Med, Asuncion, Paraguay
关键词
antichagasic activity; leishmanocidal activity; indazole N-oxide;
D O I
10.1016/j.bmc.2006.01.007
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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.
引用
收藏
页码:3467 / 3480
页数:14
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