Biological and chemical study of fused tri- and tetracyclic indazoles and analogues with important antiparasitic activity

Conformational mode adopted by compound 1 into the Trypanosoma cruzi trypanothione reductase active site. [Display omitted] ► In this study we characterized the electrochemistry mechanism of tetracylic indazoles. The radicals species generated were register using electron spin resonance spectroscopy...

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Bibliographic Details
Published in:Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy Molecular and biomolecular spectroscopy, 2012-09, Vol.95, p.670-678
Main Authors: Díaz-Urrutia, Christian A., Olea-Azar, Claudio A., Zapata, Gerald A., Lapier, Michel, Mura, Francisco, Aguilera-Venegas, Benjamín, Arán, Vicente J., López-Múñoz, Rodrigo A., Maya, Juan D.
Format: Article
Language:English
Subjects:
Cyclic voltammetry
ESR
Free radicals
Tetracyclic indazoles
Theoretical calculations
Trypanocidal activity
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Summary:Conformational mode adopted by compound 1 into the Trypanosoma cruzi trypanothione reductase active site. [Display omitted] ► In this study we characterized the electrochemistry mechanism of tetracylic indazoles. The radicals species generated were register using electron spin resonance spectroscopy. This family was also evaluated as potential tripanocide. A series of fused tri- and tetracyclic indazoles and analogues compounds (NID) with potential antiparasitic effects were studied using voltamperometric and spectroscopic techniques. Nitroanion radicals generated by cyclic voltammetry were characterized by electron spin resonance spectroscopy (ESR) and their spectral lines were explained and analyzed using simulated spectra. In addition, we examined the interaction between radical species generated from nitroindazole derivatives and glutathione (GSH). Biological assays such as activity against Trypanosoma cruzi and cytotoxicity against macrophages were carried out. Finally, spin trapping and molecular modeling studies were also done in order to elucidate the potentials action mechanisms involved in the trypanocidal activity.
ISSN:1386-1425
DOI:10.1016/j.saa.2012.04.076