Abstract
Abstract A new approach, ketone derivatization, for introducing desired functionality into the α-keto pyrophosphate analogues oxophosphonoacetic acid (COPAA) and oxomethanediphosphonic acid (COMDP) is exemplified in the synthesis of several COPAA and COMDP hydrazones with specific functional groups. The preparation of tetraalkyl COMDP esters is also described. Inhibition of HIV-1 reverse transcriptase (isolated enzyme) and of p24 production by HIV-1 (virus-infected H9 cells) by hydrazone derivatives of COPAA and COMDP is briefly discussed.
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