Ballatore C, McGuigan C, De Clercq E, Balzarini J
Welsh School of Pharmacy, Cardiff University, UK.
Bioorg Med Chem Lett. 2001 Apr 23;11(8):1053-6. doi: 10.1016/s0960-894x(01)00128-7.
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.
