Abstract
An efficient method for the synthesis of N 9-[3-fluoro-2-(phosphonomethoxy)propyl] (FPMP) derivatives of purine bases has been developed. Both ( R)- and ( S)-enantiomers of the N 6 -substituted FPMP derivatives of adenine and 2,6-diaminopurine were prepared and their anti-human immunodeficiency virus (HIV) and anti-Moloney murine sarcoma virus (MSV) activity was evaluated. Whereas none of the 6-substituted FPMPA derivatives showed any antiviral activity, several FPMPDAP derivatives had a moderate antiretroviral activity. Moreover, the data obtained from the study of the substrate activity of the active derivatives towards N 6-methyl-AMP aminohydrolase support the notion that the studied N 6-substituted FPMPDAP derivatives act as prodrugs of the antiretroviral FPMPG analogues.
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