2. Academic Validation
  3. Simple mono-derivatisation of the aryl moiety of D4A and DDA-based phosphoramidate prodrugs significantly enhances their anti-HIV potency in cell culture

Simple mono-derivatisation of the aryl moiety of D4A and DDA-based phosphoramidate prodrugs significantly enhances their anti-HIV potency in cell culture

  • Bioorg Med Chem Lett. 1999 Sep 6;9(17):2555-60. doi: 10.1016/s0960-894x(99)00416-3.
A Q Siddiqui 1,  C McGuigan,  C Ballatore,  O Wedgwood,  E De Clercq,  J Balzarini
Affiliations

Affiliation

  • 1 Welsh School of Pharmacy, Cardiff University, UK.
PMID: 10498207 DOI: 10.1016/s0960-894x(99)00416-3
Abstract

Simple mono-derivatisation of the aryl moiety of some phosphoramidate pronucleotide derivatives of d4A and ddA served to increase the lipophilicity of these membrane-soluble prodrugs. A concomitant and significant enhancement of potency against HIV-1 and HIV-2 in vitro was observed for the ddA- and d4A-based prodrugs compared to the original underivatised prodrugs.

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