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

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

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被引用次数: 21

摘要

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.