Artículo
Click chemistry decoration of amino sterols as promising strategy to developed new leishmanicidal drugs.
Porta, Exequiel Oscar Jesús
; Carvalho, Paulo B.; Avery, Mitchell A.; Tekwani, Babu L.; Labadie, Guillermo Roberto
Fecha de publicación:
01/2014
Editorial:
Elsevier Science Inc
Revista:
Steroids
ISSN:
0039-128X
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
A series of 1,2,3-triazolylsterols was prepared from pregnenolone through reductive amination and copper(I)-catalyzed azide-alkyne cycloaddition (click chemistry). The newly generated stereocenter of the key propargylamino intermediate provided a mixture of diastereomers which were separated chromatographically, and the configuration of the R isomer was determined by X-ray crystallography. Ten triazolyl sterols were prepared, and the products and intermediates were screened in vitro against different parasites, with some compounds presenting IC50 values in the low micromolar range against Leishmania donovani
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Articulos(IQUIR)
Articulos de INST.DE QUIMICA ROSARIO
Articulos de INST.DE QUIMICA ROSARIO
Citación
Porta, Exequiel Oscar Jesús; Carvalho, Paulo B.; Avery, Mitchell A.; Tekwani, Babu L.; Labadie, Guillermo Roberto; Click chemistry decoration of amino sterols as promising strategy to developed new leishmanicidal drugs.; Elsevier Science Inc; Steroids; 79; 1-2014; 28-36
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