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[Synthesis and antiherpes activity of acyclovir phosphoesters]
G A Galegov1, V M Shobukhov, N A Leont'eva
1Ivanovskii Institute of Virology, Russian Academy of Medical Sciences, Moscow, Russia.
Bioorganicheskaia Khimiia
|March 28, 1998
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.