Synthesis and evaluation of antioxidant and trypanocidal properties of a selected series of coumarin derivatives

Author:

Guíñez Roberto Figueroa1,Matos Maria João2,Vazquez-Rodriguez Saleta3,Santana Lourdes3,Uriarte Eugenio3,Olea-Azar Claudio1,Maya Juan Diego4

Affiliation:

1. Departamento de Química Inorgánica y Analítica, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Casilla 233, Santiago, Chile

2. Departamento de Química Orgánica, Facultad de Farmacia, Universidad de Santiago de Compostela, Campus Vida s/n, 15782, Santiago de Compostela, España.

3. Departamento de Química Orgánica, Facultad de Farmacia, Universidad de Santiago de Compostela, Campus Vida s/n, 15782, Santiago de Compostela, España

4. Departamento de Farmacología Molecular y Clínica, Facultad de Medicina, Universidad de Chile, Santiago, Chile

Abstract

This article describes the preparation and characterization of a selected series of coumarin derivatives with the aim of evaluating their antioxidant properties and their activity against Trypanosoma cruzi, the parasite responsible for Chagas disease. All the derivatives demonstrated moderate trypanocidal activity in the epimastigote and trypomastigote stages (clone Dm28c), with Compound 3 presenting the highest trypanocidal activity of the entire series, displaying higher activity than nifurtimox, which was used as a reference compound. In addition to the trypanocidal activity, this compound proved to have a very interesting antioxidant profile, as well as no cytotoxicity. These preliminary findings encouraged the authors to study the future structural optimization of this scaffold.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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