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Monoval-LdC: efficient prodrug of 2'-deoxy-beta-L-cytidine (L-dC), a potent and selective anti-HBV agent
S Benzaria1, C Pierra, D Bardiot
1Laboratoire Coopératif Idenix-CNRS-Université Montpellier II, CC 008, Montpellier, France.
Nucleosides, Nucleotides & Nucleic Acids
|October 21, 2003
Abstract:
In order to improve the oral bioavailability of LdC, valinyl esters were prepared as prodrugs. We report here the syntheses of the 3'-mono-, 5'-mono, and 3',5'-di-O-valinyl esters of LdC. The comparison of their ease of synthesis, their physicochemical properties, as well as their pharmacokinetic parameters in cynomologus monkeys has revealed 3'-mono-O-valinyl derivative as the most promising of the studied prodrugs. This compound is being developed as a new anti-HBV agent.
