Bioorganic & Medicinal Chemistry Letters

Application of the “trimethyl lock” 1 to Ganciclovir, a pro-prodrug with increased oral bioavailability

MP Dillon, H Cai, H Maag

Index: Dillon, Michael P.; Cai, Haiying; Maag, Hans Bioorganic and Medicinal Chemistry Letters, 1996 ,  vol. 6,  # 14  p. 1653 - 1656

Full Text: HTML

Citation Number: 21

Abstract

The synthesis and oral bioavailability of two potential prodrugs of Ganciclovir (1) based on the “trimethyl lock” is described. The mono-3-(2′-Acetoxy-4′ 6′-dimethylphenyl)-3, 3- dimethylpropanoic ester (2) showed a four-fold increase in oral bioavailability over the parent drug in rats.