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Artículo

Synthesis and biological evaluation of new quinoline derivatives as antileishmanial and antitrypanosomal agents

Chanquia, Santiago NahuelIcon ; Larregui, Facundo; Puente, Vanesa RocíoIcon ; Labriola, Carlos AlbertoIcon ; Lombardo, Maria ElisaIcon ; Garcia Liñares, Guadalupe EugeniaIcon
Fecha de publicación: 03/2019
Editorial: Academic Press Inc Elsevier Science
Revista: Bioorganic Chemistry
ISSN: 0045-2068
Idioma: Inglés
Tipo de recurso: Artículo publicado
Clasificación temática:
Química Orgánica

Resumen

As a part of our project aimed at developing new safe chemotherapeutic agents against tropical diseases, a series of aryl derivatives of 2- and 3-aminoquinoline, some of them new compounds, was designed, synthesized, and evaluated as antiproliferative agents against Trypanosoma cruzi, the parasite responsible for American trypanosomiasis (Chagas’ disease), and Leishmania mexicana, the etiological agent of Leishmaniasis. Some of them showed a remarkable activity as parasite growth inhibitors. Fluorine-containing derivatives 11b and 11c were more than twice more potent than geneticin against intracellular promastigote form of Leishmania mexicana exhibiting both IC 50 values of 41.9 μM. The IC 50 values corresponding to fluorine and chlorine derivatives 11b–d were in the same order than benznidazole against epimastigote form. These drugs are interesting examples of effective antiparasitic agents with outstanding potential not only as lead drugs but also to be used for further in vivo studies. In addition, the obtained compounds showed no toxicity in Vero cells, which makes them good candidates to control tropical diseases. Regarding the probable mode of action, assayed quinoline derivatives interacted with hemin, inhibiting its degradation and generating oxidative stress that is not counteracted by the antioxidant defense system of the parasite.
Palabras clave: CHAGAS' DISEASE , HEMIN INTERACTION , LEISHMANIASIS , OXIDATIVE DAMAGE , QUINOLINE DERIVATIVES
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info:eu-repo/semantics/restrictedAccess Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Creative Commons Attribution-NonCommercial-ShareAlike 2.5 Unported (CC BY-NC-SA 2.5)
Identificadores
URI: http://hdl.handle.net/11336/96109
URL: https://www.sciencedirect.com/science/article/pii/S0045206818310721
DOI: https://doi.org/10.1016/j.bioorg.2018.10.053
Colecciones
Articulos(UMYMFOR)
Articulos de UNID.MICROANAL.Y MET.FISICOS EN QUIM.ORG.(I)
Articulos(CIPYP)
Articulos de CENTRO DE INVEST. SOBRE PORFIRINAS Y PORFIRIAS
Articulos(IIBBA)
Articulos de INST.DE INVEST.BIOQUIMICAS DE BS.AS(I)
Citación
Chanquia, Santiago Nahuel; Larregui, Facundo; Puente, Vanesa Rocío; Labriola, Carlos Alberto; Lombardo, Maria Elisa; et al.; Synthesis and biological evaluation of new quinoline derivatives as antileishmanial and antitrypanosomal agents; Academic Press Inc Elsevier Science; Bioorganic Chemistry; 83; 3-2019; 526-534
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