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Synthesis and in vitro evaluation of a phosphonate prodrug: bis(pivaloyloxymethyl)
J E Starrett1, D R Tortolani, M J Hitchcock
1Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492.
Antiviral Research
|September 11, 1992
Abstract:
9-(2-Phosphonylmethoxyethyl)adenine (PMEA; 1) was acylated with chloromethyl pivalate to afford bis(pivaloyloxymethyl) PMEA (2). The ester prodrug demonstrated enhanced in vitro potency against HSV-2 greater than 150-fold higher than the parent compound. The antiviral activity of 2 was 50-fold better than PMEA against HSV-1, and equipotent against HIV and HCMV. The toxicity of 2 was studied in both resting and growing cells.