Synthesis and trypanocidal activity of novel benzimidazole derivatives
Copyright policy )Synthesis and trypanocidal activity of novel benzimidazole derivatives
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).
- National Autonomous University of Mexico Mexico
- University of California, San Diego United States
- Mexican Social Security Institute Mexico
- Universidad Juárez del Estado de Durango Mexico
Inhibitory Concentration 50, Mice, Antiparasitic Agents, Molecular Structure, Trypanosoma cruzi, Animals, Humans, Benzimidazoles
Inhibitory Concentration 50, Mice, Antiparasitic Agents, Molecular Structure, Trypanosoma cruzi, Animals, Humans, Benzimidazoles
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