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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:18

Article

Hornillos, Valentin^1,2  Carrillo, Eugenia³  Rivas, Luis³  Amat-Guerri, Francisco¹  Acuna, A. Ulises² 

[1] CSIC, Inst Quim Organ, E-28006 Madrid, Spain

[2] CSIC, Inst Quim Fis Rocasolano, E-28006 Madrid, Spain

[3] CSIC, Ctr Invest Biol, Madrid 28040, Spain

关键词: Miltefosine;    Hexadecylphosphocholine;    Leishmaniasis;    Parasiticide;    BODIPY;    Fluorescent lipids;   

DOI  :  10.1016/j.bmcl.2008.10.089

来源: Elsevier

【 摘 要 】

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. (C) 2008 Elsevier Ltd. All rights reserved.

【 授权许可】

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