Bioorganic & Medicinal Chemistry Letters 2008-12-15

Synthesis of BODIPY-labeled alkylphosphocholines with leishmanicidal activity, as fluorescent analogues of miltefosine.

Valentín Hornillos, Eugenia Carrillo, Luis Rivas, Francisco Amat-Guerri, A Ulises Acuña

Index: Bioorg. Med. Chem. Lett. 18 , 6336-9, (2008)

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Abstract

Two general synthetic methods are described, by which the highly fluorescent and photostable BODIPY group can be inserted in and aligned with the alkyl backbone of linear lipids. These methods have been used to prepare strongly emitting analogues of the leishmanicidal drug miltefosine, in which the antiparasite activity in vitro of the original drug is preserved.