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 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.
Siddiqui
A Q
AQ
Welsh School of Pharmacy, Cardiff University, UK.
McGuigan
C
C
Ballatore
C
C
Wedgwood
O
O
De Clercq
E
E
Balzarini
J
J
D019380:Anti-HIV Agents / Q000737:chemistry* / Q000494:pharmacology*; D002478:Cells, Cultured; D016048:Dideoxyadenosine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects; D015498:HIV-2 / Q000187:drug effects; D006801:Humans; D013329:Structure-Activity Relationship
D019380:Anti-HIV Agents; D016048:Dideoxyadenosine; C075923:2'3'-didehydro-2'3'-dideoxyadenosine