Bioorganicheskaia khimiia 1997-11-01

[Synthesis and antiherpes activity of acyclovir phosphoesters].

G A Galegov, V M Shobukhov, N A Leont'eva, M V Ias'ko

Index: Bioorg. Khim. 23(11) , 906-9, (1997)

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Abstract

9-(Hydroxyethyloxymethyl)guanine (acyclovir) phosphite and fluorophosphate were synthesized by the reactions of acyclovir with phosphorus trichloride in triethyl phosphate and with fluorophosphoric acid in the presence of 2,4,6-triisopropylbenzenesulfonyl chloride, respectively, and characterized by the data of 1H and 31P NMR and mass spectra. These products selectively inhibit reproduction of the herpes simplex virus type 1 in the Vero cell culture, the phosphite being also substantially active against a herpes virus strain resistant to acyclovir.