Author/Authors :
Adam Q. Siddiqui، نويسنده , , Christopher McGuigan، نويسنده , , Carlo Ballatore، نويسنده , , Orson Wedgwood، نويسنده , , Erik De Clercq، نويسنده , , Jan Balzarini، نويسنده ,
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. 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.
