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Title: Library of Selenocyanate and Diselenide Derivatives as In Vivo Antichagasic Compounds Targeting Trypanosoma cruzi Mitochondrion.
Authors: Martín-Escolano, Rubén
Molina-Carreño, Daniel
Plano, Daniel
Espuelas, Socorro
Rosales, María J
Moreno, Esther
Aydillo, Carlos
Sanmartín, Carmen
Sánchez-Moreno, Manuel
Marín, Clotilde
Keywords: American trypanosomiasis;Trypanosoma cruzi;chagas disease;chemotherapy;drug discovery;neglected tropical diseases;screening cascade;selenium derivatives;target product profile
Issue Date: 1-May-2021
Abstract: Chagas disease is usually caused by tropical infection with the insect-transmitted protozoan Trypanosoma cruzi. Currently, Chagas disease is a major public health concern worldwide due to globalization, and there are no treatments neither vaccines because of the long-term nature of the disease and its complex pathology. Current treatments are limited to two obsolete drugs, benznidazole and nifurtimox, which lead to serious drawbacks. Taking into account the urgent need for strict research efforts to find new therapies, here, we describe the in vitro and in vivo trypanocidal activity of a library of selected forty-eight selenocyanate and diselenide derivatives that exhibited leishmanicidal properties. The inclusion of selenium, an essential trace element, was due to the well-known extensive pharmacological activities for selenium compounds including parasitic diseases as T. cruzi. Here we present compound 8 as a potential compound that exhibits a better profile than benznidazole both in vitro and in vivo. It shows a fast-acting behaviour that could be attributed to its mode of action: it acts in a mitochondrion-dependent manner, causing cell death by bioenergetic collapse. This finding provides a step forward for the development of a new antichagasic agent.
metadata.dc.identifier.doi: 10.3390/ph14050419
ISSN: 1424-8247
Appears in Collections:Producción 2020

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