Design and Synthesis of Organophosphorus Compounds with Antiviral and Other Bioactivities

Design and Synthesis of α-Carboxy Nucleoside Phosphonate Analogues and Evaluation as HIV-1 Reverse Transcriptase-Targeting Agents

“…McKenna et al later synthesized a range of halogen- and methyl-substituted derivatives of PAA, a number of which were found to possess potent anti(retro)viral activity. Interestingly, the carbonyl derivative 10 was significantly more active than 9 . The attachment of PAA and PFA by ester and amide linkages to the 5′- O and N - positions of 3TC has been reported, but the resulting derivatives were less active against HIV-1 than the parent compound …”

“…Interestingly, the carbonyl derivative 10 was significantly more active than 9. 32 The attachment of PAA and PFA by ester and amide linkages to the 5′-O and N-positions of 3TC has been reported, but the resulting derivatives were less active against HIV-1 than the parent compound. 33 In general, phosphononucleoside research involves compounds bearing a simple CH 2 PO(OH) 2 substituent.…”