Detalle Publicación

Antichagasic profile of a Series of Mannich Base-Type Derivatives: Design, Synthesis, in vitro Evaluation, and Computational Studies Involving Iron Superoxide Dismutase
Autores: Paucar Bernabé, Rocio Valeria; Martin-Escolano, R.; Moreno de Viguri, Elsa; Cirauqui, N.; Marin, C.; Sanchez-Moreno, M. ; Pérez Silanes, Silvia (Autor de correspondencia)
Título de la revista: CHEMISTRYSELECT
ISSN: 2365-6549
Volumen: 4
Número: 27
Páginas: 8112 - 8121
Fecha de publicación: 2019
Lugar: WOS
Chagas disease is a silent disease that continues to endanger millions of people and, due to its insufficient current chemotherapy, urgently requires the development of more effective drugs. With this objective, twenty-six Mannich base derivatives were synthesized, and their in vitro activity was evaluated against Trypanosoma cruzi. Three out of the twenty-six compounds showed interesting results, including IC50 valuesT. cruzi strains. In addition, these compounds showed similar infection rates in Vero cells compared to those of benznidazole at 50 mu M. Finally, some studies were performed to investigate the possible mechanism of action; moreover, computational studies proposed a binding mode of these derivatives to Fe-SOD. This new series of compounds has an encouraging antichagasic profile with a simplified structure and synthetic routes. Therefore, the most active compounds should be considered as leads for further optimization of the antichagasic activity.