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

Bioorg Med Chem Lett

Medicinal Chemistry, Department of Pharmaceutical Sciences, Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat-10, 3000 Leuven, Belgium. Electronic address:

Published: February 2014

AI Article Synopsis

  • A new series of phospholipid prodrugs derived from dideoxy nucleosides has been created and tested for effectiveness against HIV.
  • The study found that the biological activity increased significantly, by a factor of 500, but only for the adenine nucleoside.
  • This indicates that the prodrug strategy is selective and works differently based on the specific nucleobase used.

Article 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.

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http://dx.doi.org/10.1016/j.bmcl.2013.12.093DOI Listing

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