Hydroxy fatty acids for the delivery of dideoxynucleosides as anti-HIV agents

Bioorg Med Chem Lett. 2014 Feb 1;24(3):817-20. doi: 10.1016/j.bmcl.2013.12.093.

Kishore Lingam Gangadhara ¹, Eveline Lescrinier ¹, Christophe Pannecouque ², Piet Herdewijn ³

Affiliations

1 Medicinal Chemistry, Department of Pharmaceutical Sciences, Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat-10, 3000 Leuven, Belgium.
2 Laboratory of Virology and Chemotherapy, Department of Microbiology and Immunology, Rega Institute for Medical Research, KU Leuven, Kapucijnenvoer 33, 3000 Leuven, Belgium.
3 Medicinal Chemistry, Department of Pharmaceutical Sciences, Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat-10, 3000 Leuven, Belgium. Electronic address: [email protected].

PMID: 24411122 DOI: 10.1016/j.bmcl.2013.12.093

Abstract

A series of α- and β-carboxylated phospholipid prodrugs of dideoxy nucleosides have been synthesized and evaluated against HIV. An increase in biological effect with a factor of 500 has only been observed for the adenine nucleoside, which suggests that this prodrug approach is base specific.

Keywords

HIV; Nucleotides; Phospholipids; Prodrugs; d4A.

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