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Título

Synthesis of 16-mercaptohexadecylphosphocholine, a miltefosine analog with leishmanicidal activity

AutorHornillos, Valentín ; Saugar, José María; García de la Torre, Beatriz; Andreu, David; Acuña, A. Ulises
Palabras claveAlkylphosphocholine miltefosine
Leishmaniasis
Fecha de publicación1-oct-2006
EditorElsevier
CitaciónBioorganic Medicinal Chem. Lett.,16, 5190-5193 (2006)
ResumenThe alkylphosphocholine miltefosine (n-hexadecylphosphocholine, MT) has been introduced recently as a very effective drug for the oral treatment of human leishmaniasis. However, the parasiticidal mechanism of MT at a molecular level is far from being understood. Here we report the synthesis and biological characterization of 16-mercaptohexadecylphosphocholine, a thiol analog of MT which was designed to facilitate the search of MT interacting targets within the parasite by a variety of analytical methods. This analog presents the same leishmanicidal effect as the parent drug against Leishmania donovani promastigotes and Leishmania pifanoi axenic amastigotes, and has been used to develop an affinity chromatography method to attempt the isolation of putative Leishmania proteins that bind to the phosphocholine part of the molecule.
Versión del editorhttp://dx.doi.org/10.1016/j.bmcl.2006.07.004
URIhttp://hdl.handle.net/10261/11616
DOI10.1016/j.bmcl.2006.07.004
ISSN0960-894X
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