Synthesis and evaluation of novel amidate prodrugs of PMEA and PMPA

Bioorganic & Medicinal Chemistry Letters
2001.0

Abstract

Some novel amidate prodrugs of PMEA and PMPA have been synthesised and tested in vitro for their biological activity. Compound 5 in particular showed greatly enhanced antiviral potency compared with the parent nucleotide analogue. In vitro enzymatic studies and structure-activity relationships indicate that the degradation mechanism of such prodrugs may be the same as that described for the phosphoramidate triesters of nucleotide analogues.

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