Antichagasic profile of a Series of Mannich Base‐Type Derivatives: Design, Synthesis, in vitro Evaluation, and Computational Studies Involving Iron Superoxide Dismutase

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 ev...

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Veröffentlicht in:ChemistrySelect (Weinheim) 2019-07, Vol.4 (27), p.8112-8121
Hauptverfasser: Paucar, Rocío, Martín‐Escolano, Rubén, Moreno‐Viguri, Elsa, Cirauqui, Nuria, Marín, Clotilde, Sánchez‐Moreno, Manuel, Pérez‐Silanes, Silvia
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Sprache:eng
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Zusammenfassung: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 values21. In addition, these compounds could be considered as selective inhibitors of the enzyme Fe‐SOD. Also, docking studies proposed the binding mode of these derivatives to Fe‐SOD enzyme. Therefore, additional studies should be considered to optimize the antichagasic profile of these compounds.
ISSN:2365-6549
2365-6549
DOI:10.1002/slct.201901108