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

Díaz-Urrutia, Christian; Olea‐Azar, Claudio; Zapata, Gerald; Lapier, Michel; Mura, Francisco; Aguilera‐Venegas, Benjamín; Arán, Vicente J.; López‐Muñoz, Rodrigo; Maya, Juan Diego

doi:10.1016/j.saa.2012.04.076

Cited by 13 publications

(4 citation statements)

References 32 publications

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“…Both BZN and NFX are unable to provide a definitive cure for Chagas due to several limitations, such as strong adverse events, and both medicines are more effective only in the early stages of the disease but not in its chronic phase. Resistance of several Chagas strains against treatment was observed as well [3], and the poor solubility of these drugs in water is a serious difficulty for their practical use [4]. We focus on BZN in this work as it is the preferred choice due to the severe NFX gastrointestinal and neurological side effects.…”

Section: Introductionmentioning

confidence: 99%

Optical Absorption of the Antitrypanocidal Drug Benznidazole inWater

et al. 2014

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UV-vis optical absorption spectra of the antitrypanocidal drug benznidazole solvated in water were measured for various concentrations. The spectra show a prominent peak around 3.80 eV, while deconvolution of the UV-vis optical absorption spectra revealed six bands centered at 3. 60, 3.83, 4.15, 4.99, 5.60, and 5.76 eV. Benznidazole electronic transitions were obtained after density functional theory (DFT) calculations within the polarized continuum (PCM) model for water solvation. Molecular geometry optimizations were carried out, and the measured absorption peaks were related to specific molecular orbital transitions obtained within the time dependent DFT (TD-DFT) with excellent agreement between theory and experiment.

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Section: Introductionmentioning

confidence: 99%

Optical Absorption of the Antitrypanocidal Drug Benznidazole inWater

et al. 2014

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“…The treatment of this disease is complicated: benznidazole and nifurtimox are the only available drugs, and both produce severe side effects [3]. The search for new treatments against this parasite is an on-going topic for research [4–7]. …”

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confidence: 99%

Differential Effects of Two Widely Used Solvents, DMSO and Ethanol, on the Growth and Recovery of Trypanosoma cruzi Epimastigotes in Culture

Cevallos¹,

Herrera²,

López‐Villaseñor³

et al. 2017

Korean J Parasitol

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Trypanosoma cruzi is the etiological agent of Chagas disease. Epimastigote forms of T. cruzi can be readily cultured in axenic conditions. Ethanol and dimethyl sulfoxide (DMSO) are commonly used solvents employed as vehicles for hydrophobic compounds. In order to produce a reference plot of solvent dependent growth inhibition for T. cruzi research, the growth of epimastigotes was analyzed in the presence of different concentrations of ethanol (0.1–4.0%) and DMSO (0.5–7.5%). The ability of the parasites to resume growth after removal of these solvents was also examined. As expected, both ethanol and DMSO produced a dose-dependent inhibition of cellular growth. Parasites could recover normal growth after 9 days in up to 2% ethanol or 5% DMSO. Since DMSO was better tolerated than ethanol, it is thus recommended to prefer DMSO over ethanol in the case of a similar solubility of a given compound.

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“…In addition, the interaction between radical species generated from nitroindazole derivatives and glutathione was examined. Finally, spin trapping and molecular modeling studies were performed in order to elucidate the potentials action mechanisms involved in the trypanocidal activity and the target/s involved [658]. b.…”

Section: Novel Anti T Cruzi Activities With Known Single or Multi Tar...mentioning

confidence: 99%

Targets and Patented Drugs for Chemotherapy of Chagas Disease in the Last 15 Years-Period

Duschak

2016

PRI

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In summary, loans on anti-Chagas disease agents focused to specific parasite targets as their metabolic pathways or specific enzymes will be summarized. Targets will also be specifically discussed. Patent literature collected and published from 2000 to 2015, alleging inhibitors for specific T. cruzi targets or trypanocidal activity was achieved over the search database from Delphion Research intellectual property network including international patents and the European patent office, Espacenet.

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

Cited by 13 publications

References 32 publications

Optical Absorption of the Antitrypanocidal Drug Benznidazole inWater

Optical Absorption of the Antitrypanocidal Drug Benznidazole inWater

Differential Effects of Two Widely Used Solvents, DMSO and Ethanol, on the Growth and Recovery of Trypanosoma cruzi Epimastigotes in Culture

Targets and Patented Drugs for Chemotherapy of Chagas Disease in the Last 15 Years-Period

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