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Title: In vitro antileishmanial activity and iron superoxide dismutase inhibition of arylamine Mannich base derivatives.
Authors: Martin-Montes, Alvaro
Santivañez-Veliz, Mery
Moreno-Viguri, Elsa
Martín-Escolano, Rubén
Jiménez-Montes, Carmen
Lopez-Gonzalez, Catalina
Marín, Clotilde
Sanmartín, Carmen
Gutiérrez Sánchez, Ramón
Sánchez-Moreno, Manuel
Pérez-Silanes, Silvia
Keywords: Leishmania braziliensis;Leishmania donovani;Leishmania infantum;Mannich base derivatives;arylamine derivatives;iron superoxide dismutase
metadata.dc.subject.mesh: Animals
Cell Line
Leishmania braziliensis
Leishmania donovani
Leishmania infantum
Mannich Bases
Parasitic Sensitivity Tests
Superoxide Dismutase
Trypanocidal Agents
Issue Date: 9-Aug-2017
Abstract: Leishmaniasis is one of the world's most neglected diseases, and it has a worldwide prevalence of 12 million. There are no effective human vaccines for its prevention, and treatment is hampered by outdated drugs. Therefore, research aiming at the development of new therapeutic tools to fight leishmaniasis remains a crucial goal today. With this purpose in mind, we present 20 arylaminoketone derivatives with a very interesting in vitro and in vivo efficacy against Trypanosoma cruzi that have now been studied against promastigote and amastigote forms of Leishmania infantum, Leishmania donovani and Leishmania braziliensis strains. Six out of the 20 Mannich base-type derivatives showed Selectivity Index between 39 and 2337 times higher in the amastigote form than the reference drug glucantime. These six derivatives affected the parasite infectivity rates; the result was lower parasite infectivity rates than glucantime tested at an IC25 dose. In addition, these derivatives were substantially more active against the three Leishmania species tested than glucantime. The mechanism of action of these compounds has been studied, showing a greater alteration in glucose catabolism and leading to greater levels of iron superoxide dismutase inhibition. These molecules could be potential candidates for leishmaniasis chemotherapy.
metadata.dc.identifier.doi: 10.1017/S0031182017001123
Appears in Collections:Producción 2020

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