Ce. Mckenna et al., SYNTHESIS AND HIV-1 REVERSE-TRANSCRIPTASE INHIBITION-ACTIVITY OF FUNCTIONALIZED PYROPHOSPHATE ANALOGS, Phosphorus, sulfur and silicon and the related elements, 76(1-4), 1993, pp. 399-402
A new approach, ketone derivatization, for introducing desired functio
nality into the alpha-keto pyrophosphate analogues oxophosphonoacetic
acid (COPAA) and oxomethanediphosphonic acid (COMDP) is exemplified in
the synthesis of several COPAA and COMDP hydrazones with specific fun
ctional groups. The preparation of tetraalkyl COMDP esters is also des
cribed. Inhibition of HIV-1 reverse transcriptase (isolated enzyme) an
d of p24 production by HIV-1 (virus-infected H9 cells) by hydrazone de
rivatives of COPAA and COMDP is briefly discussed.