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Article

Library of Selenocyanate and Diselenide Derivatives as In Vivo Antichagasic Compounds Targeting Trypanosoma cruzi Mitochondrion

1
Laboratory of Molecular & Evolutionary Parasitology, RAPID Group, School of Biosciences, University of Kent, Canterbury CT2 7NJ, UK
2
Department of Parasitology, Instituto de Investigación Biosanitaria (ibs.Granada), Hospitales Universitarios de Granada/University of Granada, Severo Ochoa s/n, 18071 Granada, Spain
3
Facultad de Farmacia y Nutrición, Departamento de Tecnología y Química Farmacéuticas, Universidad de Navarra, Irunlarrea, E-31008 Pamplona, Spain
4
Instituto de Salud Tropical, Universidad de Navarra, ISTUN, Irunlarrea, E-31008 Pamplona, Spain
5
Instituto de Investigaciones Sanitarias de Navarra (IdiSNA) Irunlarrea, E-31008 Pamplona, Spain
*
Authors to whom correspondence should be addressed.
Academic Editor: Marcelo J. Nieto
Pharmaceuticals 2021, 14(5), 419; https://0-doi-org.brum.beds.ac.uk/10.3390/ph14050419
Received: 24 March 2021 / Revised: 23 April 2021 / Accepted: 26 April 2021 / Published: 1 May 2021
(This article belongs to the Special Issue Antiparasitics)
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. View Full-Text
Keywords: American trypanosomiasis; chagas disease; chemotherapy; drug discovery; neglected tropical diseases; screening cascade; selenium derivatives; target product profile; Trypanosoma cruzi American trypanosomiasis; chagas disease; chemotherapy; drug discovery; neglected tropical diseases; screening cascade; selenium derivatives; target product profile; Trypanosoma cruzi
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MDPI and ACS Style

Martín-Escolano, R.; Molina-Carreño, D.; Plano, D.; Espuelas, S.; Rosales, M.J.; Moreno, E.; Aydillo, C.; Sanmartín, C.; Sánchez-Moreno, M.; Marín, C. Library of Selenocyanate and Diselenide Derivatives as In Vivo Antichagasic Compounds Targeting Trypanosoma cruzi Mitochondrion. Pharmaceuticals 2021, 14, 419. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14050419

AMA Style

Martín-Escolano R, Molina-Carreño D, Plano D, Espuelas S, Rosales MJ, Moreno E, Aydillo C, Sanmartín C, Sánchez-Moreno M, Marín C. Library of Selenocyanate and Diselenide Derivatives as In Vivo Antichagasic Compounds Targeting Trypanosoma cruzi Mitochondrion. Pharmaceuticals. 2021; 14(5):419. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14050419

Chicago/Turabian Style

Martín-Escolano, Rubén, Daniel Molina-Carreño, Daniel Plano, Socorro Espuelas, María J. Rosales, Esther Moreno, Carlos Aydillo, Carmen Sanmartín, Manuel Sánchez-Moreno, and Clotilde Marín. 2021. "Library of Selenocyanate and Diselenide Derivatives as In Vivo Antichagasic Compounds Targeting Trypanosoma cruzi Mitochondrion" Pharmaceuticals 14, no. 5: 419. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14050419

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