Bompart, Daznia; Núñez Durán, Jorge; Rodríguez, Daniel; Kouznetsov, Vladimir V.; Meléndez Gómez, Carlos M.; Sojo, Felipe; Arvelo, Francisco; Visbal, Gonzalo; Álvarez, Álvaro; Serrano Martín, Xenón; García Marchán, Yael (2013-05-09)
Abstract:A series of diverse simple C2-aryl quinolines was synthesized de novo via a straightforward synthesis based on the acid-catalyzed multicomponent imino Diels–Alder reactions. Seven selected quinolines were evaluated at different stages of Leishmania braziliensis parasite. Among them, the 6-ethyl-2-phenylquinoline 5f was able to inhibit the growth of promastigotes of this parasite without affecting the mammalian cells viability and decreasing the number of intracellular L. braziliensis amastigotes on BMDM macrophages. The mechanism of action studied for the selected compound consisted in: (1) alteration of parasite bioenergetics, by disrupting mitochondrial electrochemical potential and alkalinisation of acidocalcisomes, and (2) inhibition of ergosterol biosynthetic pathway in promastigote forms. These results validate the efficiency of quinoline molecules as leishmanicide compounds.
Es proyecto?:no
Autor:Bompart, Daznia
Programa Nal. Colciencias:Programas de CT+I Ejecutados por Redes de Conocimiento
Insitución cofinanciadora:Departamento Administrativo de Ciencia, Tecnología e Innovación [CO] Colciencias
Institución participante:Bio-Red-CO-CENIVAM
Tipo de producto resultado de investigación:info:eu-repo/semantics/article
Fecha:2013-05-09
Proyecto id:5507-543-31904
Nombre de proyecto principal:Programa: Bioprospección y desarrollo de ingredientes naturales para las industrias cosmética, farmacéutica y de productos de aseo con base en la biodiversidad colombiana
Comunidad vinculada:Comunidad científica colombiana