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Structure-activity relationships and mechanistic studies of novel mitochondria-targeted, leishmanicidal derivatives of the 4-aminostyrylquinoline scaffold

AuthorsStaderini, Matteo; Piquero, Marta; Abengozar, M. A. ; Nácher-Vázquez, Montserrat ; Romanelli, Giulia; López-Alvarado, Pilar; Rivas, Luis ; Bolognesi, Maria Laura; Menéndez, J. Carlos
KeywordsLeishmanicidal compounds
Mitochondrial metabolism
Issue Date14-Mar-2019
CitationEuropean Journal of Medicinal Chemistry 171: 38-53 (2019)
AbstractA 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.
Description58 p.-6 fig.-1 tab.-5 schem.-1 graph.abst
Publisher version (URL)https://doi.org/10.1016/j.ejmech.2019.03.007
Appears in Collections:(CIB) Artículos
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