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Nucleosides and Nucleotides Volume 16, 1997 - Issue 7-9
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IV. PRECLINICAL STUDIES OF NUCLEOSIDES AND NUCLEOTIDES

The Pronucleotide Approach. III. Synthesis, Anti-HBV Activity and Stability Studies of the Bis(S-pivaloyl-2-thioethyl) Phosphotriester Derivative of Acyclovir

Gilles Valette Laboratoire de Chimie Bioorganique, UMR CNRS-USTL 5625, Université Montpellier II, case courier 008, Place E. Bataillon, 34095, Montpellier, cedex 5, FRANCE
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Jean-Luc Girardet Laboratoire de Chimie Bioorganique, UMR CNRS-USTL 5625, Université Montpellier II, case courier 008, Place E. Bataillon, 34095, Montpellier, cedex 5, FRANCE
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Alain Pompon Laboratoire de Chimie Bioorganique, UMR CNRS-USTL 5625, Université Montpellier II, case courier 008, Place E. Bataillon, 34095, Montpellier, cedex 5, FRANCE
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Christian Périgaud Laboratoire de Chimie Bioorganique, UMR CNRS-USTL 5625, Université Montpellier II, case courier 008, Place E. Bataillon, 34095, Montpellier, cedex 5, FRANCE
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Gilles Gosselin Laboratoire de Chimie Bioorganique, UMR CNRS-USTL 5625, Université Montpellier II, case courier 008, Place E. Bataillon, 34095, Montpellier, cedex 5, FRANCE
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Brent Korba Virology Branch, DMID, NIH, Solar Bldg, 6003 Executive Blvd, Bethesda, MD, 20892, USA
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Olivier Hantz Unité de Recherche sur les Hépatites, le SIDA et les Rétrovirus Humains, INSERM U 271, 151, cours Albert Thomas, 69424, Lyon, cedex 3, FRANCE
&
Jean-Louis Imbach Laboratoire de Chimie Bioorganique, UMR CNRS-USTL 5625, Université Montpellier II, case courier 008, Place E. Bataillon, 34095, Montpellier, cedex 5, FRANCE
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Pages 1331-1335 | Published online: 16 Aug 2006
 
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Abstract

The nucleoside analog Acyclovir (ACV) is used in the treatment of herpes simplex (HSV) and varicella-zoster (VZV) diseases. The possibility to extend the application field of ACV by using the bis[SATE] pronucleotide approach in order to deliver ACVMP inside the cell was investigated. And actually, the title compound has potent anti-hepatitis B activity in cell culture experiments. Here, we also report its synthesis and stability in various media.

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