IQUIR 05412
INSTITUTO DE QUIMICA ROSARIO
Unidad Ejecutora - UE
artículos
Título:
Click chemistry decoration of amino sterols as promising strategy to developed new leishmanicidal drugs
Autor/es:
EXEQUIEL O. J. PORTA; PAULO B. CARVALHO; MITCHELL A. AVERY; BABU L. TEKWANI; GUILLERMO R. LABADIE
Revista:
STEROIDS
Editorial:
ELSEVIER SCIENCE INC
Referencias:
Lugar: Amsterdam; Año: 2014 vol. 79 p. 28 - 36
ISSN:
0039-128X
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 theRisomer was determined by X-ray crystallography. Ten triazolyl sterols were prepared, and the products and intermediates were screenedin vitro against different parasites, with some compounds presenting IC50values in the low micromolar range against Leishmania donovani.
