2. Academic Validation
  3. Design, synthesis, and anti-HIV activity of 2',3'-didehydro-2',3'-dideoxyuridine (d4U), 2',3'-dideoxyuridine (ddU) phosphoramidate 'ProTide' derivatives

Design, synthesis, and anti-HIV activity of 2',3'-didehydro-2',3'-dideoxyuridine (d4U), 2',3'-dideoxyuridine (ddU) phosphoramidate 'ProTide' derivatives

  • Bioorg Med Chem Lett. 2007 Jul 1;17(13):3666-9. doi: 10.1016/j.bmcl.2007.04.043.
Youcef Mehellou 1,  Christopher McGuigan,  Andrea Brancale,  Jan Balzarini
Affiliations

Affiliation

  • 1 Welsh School of Pharmacy, Cardiff University, King Edward VII Avenue, Cardiff, UK.
PMID: 17485204 DOI: 10.1016/j.bmcl.2007.04.043
Abstract

We report the synthesis of 2',3'-didehydro-2',3'-dideoxyuridine (d4U) and 2',3'-dideoxyuridine (ddU) phosphoramidate 'ProTide' derivatives and their evaluation against HIV-1 and HIV-2. In addition, we conducted molecular modeling studies on both d4U and ddU monophosphates to investigate their second phosphorylation process. The findings from the modeling studies provide compelling evidence for the lack of anti-HIV activity of d4U phosphoramidates, in contrast with the corresponding ddU phosphoramidates.

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