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Título: | Structure-activity relationships and mechanistic studies of novel mitochondria-targeted, leishmanicidal derivatives of the 4-aminostyrylquinoline scaffold |
Autor: | Staderini, Matteo; Piquero, Marta; Abengozar, M. A. CSIC; Nácher-Vázquez, Montserrat CSIC ORCID; Romanelli, Giulia; López-Alvarado, Pilar; Rivas, Luis CSIC ORCID ; Bolognesi, Maria Laura; Menéndez, J. Carlos | Palabras clave: | Leishmanicidal compounds 4-Aminoquinolines 2-Styrylquinolines Mitochondrial metabolism |
Fecha de publicación: | 14-mar-2019 | Editor: | Elsevier | Citación: | European Journal of Medicinal Chemistry 171: 38-53 (2019) | Resumen: | A new class of quinoline derivatives, bearing amino chains at C-4 and a styryl group at C-2, were tested on Leishmania donovani promastigotes and axenic and intracellular Leishmania pifanoi amastigotes. The introduction of the C-4 substituent improves the activity, which is due to interference with the mitochondrial activity of the parasite and its concomitant bioenergetic collapse by ATP exhaustion. Some compounds show a promising antileishmanial profile, with low micromolar or submicromolar activity on promastigote and amastigote forms and a good selectivity index. | Descripción: | 58 p.-6 fig.-1 tab.-5 schem.-1 graph.abst | Versión del editor: | https://doi.org/10.1016/j.ejmech.2019.03.007 | URI: | http://hdl.handle.net/10261/178024 | DOI: | 10.1016/j.ejmech.2019.03.007 | ISSN: | 0223-5234 | E-ISSN: | 1768-3254 |
Aparece en las colecciones: | (CIB) Artículos |
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J. Med. Chem._Staderini_2019.pdf | Postprint | 2,79 MB | Adobe PDF | Visualizar/Abrir |
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