Synthesis and trypanocidal activity of novel benzimidazole derivatives

[Display omitted] The present work reports the synthesis and biological activity of a series of 14 benzimidazole derivatives designed to act on the enzyme triosephosphate isomerase of Trypanosoma cruzi (TcTIM). This enzyme is involved in the metabolism of glucose, the only source of energy for the p...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2016-09, Vol.26 (17), p.4377-4381
Main Authors: Velázquez-López, José Miguel, Hernández-Campos, Alicia, Yépez-Mulia, Lilián, Téllez-Valencia, Alfredo, Flores-Carrillo, Paulina, Nieto-Meneses, Rocío, Castillo, Rafael
Format: Article
Language:English
Subjects:
Animals
Antiparasitic Agents - chemical synthesis
Antiparasitic Agents - chemistry
Antiparasitic Agents - pharmacology
Benzimidazole derivatives
Benzimidazoles - chemical synthesis
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Chagas disease
Humans
Inhibitory Concentration 50
Mice
Molecular Structure
Triosephosphate isomerase
Trypanosoma cruzi
Trypanosoma cruzi - drug effects
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Summary:[Display omitted] The present work reports the synthesis and biological activity of a series of 14 benzimidazole derivatives designed to act on the enzyme triosephosphate isomerase of Trypanosoma cruzi (TcTIM). This enzyme is involved in the metabolism of glucose, the only source of energy for the parasite. In this study, we found four compounds that inhibit TcTIM moderately and lack inhibitory activity against human TIM (HsTIM). In vitro studies against T. cruzi epimastigotes showed two compounds that were more active than the reference drug nifurtimox, and these presented a low cytotoxic effect in mouse macrophages (J744 cell line).
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2015.08.018