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AutorTabélé, Clémence
AutorFaiões, Viviane dos S.
AutorGrimaud, Fabien
AutorSantos, Eduardo Caio Torres
AutorKhoumeri, Omar
AutorCurti, Christophe
AutorVanelle, Patrice
Fecha de acceso2018-09-18T16:27:04Z
Fecha de disponibilización2018-09-18T16:27:04Z
Fecha de publicación2018
ReferenciaTABÈLÉ, Clémence et al. Original antileishmanial hits: Variations around amidoximes. European Journal of Medicinal Chemistry, v. 148, p. 154-164, Feb. 2018.pt_BR
ISSN0223-5234pt_BR
URIhttps://www.arca.fiocruz.br/handle/icict/28868
Idiomaengpt_BR
EditorElsevierpt_BR
Derechos de autorrestricted access
Palabras clave en PortuguésCitotoxicidade in vitropt_BR
Palabras clave en PortuguésAntileishemanialpt_BR
Palabras clave en PortuguésAtividade antiprotozoária in vitropt_BR
Palabras clave en PortuguésAmidoximaspt_BR
Palabras clave en Portuguésmodulação de fármacospt_BR
TítuloOriginal antileishmanial hits: Variations around amidoximespt_BR
Tipo del documentoArticle
DOI10.1016/j.ejmech.2018.02.029
Resumen en InglésIn continuation to our previous findings on amidoximes' antiparasitic activities, a new series of 23 original derivatives was designed and obtained by convergent synthesis. First, new terminal alkenes were synthesized by cross-coupling reaction. Then, cyclization was performed between terminal alkenes and β-ketosulfones using manganese(III) acetate reactivity. Twenty-three amidoximes were tested for their in vitro activity against Leishmania amazonensis promastigotes and their toxicity on murine macrophages. Seven of the tested compounds exhibited an antileishmanial activity at lower than 10 μM with moderate to low toxicity. Six of these molecules showed activity at lower than 10 μM against promastigotes and toxicity at higher than 50 μM were selected and evaluated for their activity against intracellular Leishmania amazonensis amastigotes. Modulating chemical substituents in position 2 of dihydrofuran highly influenced their antileishmanial activities. The introduction of a methyl or trifluoromethyl group on the benzene ring of the benzyl group had a positive influence on activity without significantly increasing toxicity (52, 59, 60).pt_BR
AfiliaciónAix Marseille Université. Laboratoire de Pharmaco-Chimie Radicalaire. Faculté de Pharmacie. 27 Boulevard Jean Moulin. Marseille, France.pt_BR
AfiliaciónFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia de Tripanossomatídeos. Rio de Janeiro, RJ, Brasil.pt_BR
AfiliaciónAix Marseille Université. Laboratoire de Pharmaco-Chimie Radicalaire. Faculté de Pharmacie. 27 Boulevard Jean Moulin. Marseille, France.pt_BR
AfiliaciónFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia de Tripanossomatídeos. Rio de Janeiro, RJ, Brasil.pt_BR
AfiliaciónAix Marseille Université. Laboratoire de Pharmaco-Chimie Radicalaire. Faculté de Pharmacie. 27 Boulevard Jean Moulin. Marseille, France.pt_BR
AfiliaciónAix Marseille Université. Laboratoire de Pharmaco-Chimie Radicalaire. Faculté de Pharmacie. 27 Boulevard Jean Moulin. Marseille, France.pt_BR
AfiliaciónAix Marseille Université. Laboratoire de Pharmaco-Chimie Radicalaire. Faculté de Pharmacie. 27 Boulevard Jean Moulin. Marseille, France.pt_BR
Palavras clave en InglêsAmidoximespt_BR
Palavras clave en InglêsDihydrofuranpt_BR
Palavras clave en InglêsManganese(III) acetatept_BR
Palavras clave en InglêsPharmacomodulationpt_BR
Palavras clave en InglêsCytotoxicity in vitropt_BR
Palavras clave en InglêsAntiprotozoan activity in vitropt_BR
Palavras clave en Inglêsantileishmanial hitspt_BR
Fecha de embargo2030-01-01


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