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Monoval-LdC: efficient prodrug of 2'-deoxy-beta-L-cytidine (L-dC), a potent and selective anti-HBV agent. 2003
S Benzaria, and
C Pierra, and
D Bardiot, and
E Cretton-Scott, and
E G Bridges, and
X J Zhou, and
D Standring, and
G Gosselin
Laboratoire Coopératif Idenix-CNRS-Université Montpellier II, CC 008, Montpellier, France.
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.
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