单酯-LdC：2'-脱氧-β-L-胞苷（L-dC）的高效前药，一种强效且选择性的抗乙肝病毒药物。
Monoval-LdC: efficient prodrug of 2'-deoxy-beta-L-cytidine (L-dC), a potent and selective anti-HBV agent.
作者信息
Benzaria S, Pierra C, Bardiot D, Cretton-Scott E, Bridges E G, Zhou X J, Standring D, Gosselin G
机构信息
Laboratoire Coopératif Idenix-CNRS-Université Montpellier II, CC 008, Montpellier, France.
出版信息
Nucleosides Nucleotides Nucleic Acids. 2003 May-Aug;22(5-8):1003-6. doi: 10.1081/NCN-120022723.
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.
为了提高LdC的口服生物利用度，制备了缬氨酰酯作为前药。我们在此报告LdC的3'-单-、5'-单-和3',5'-二-O-缬氨酰酯的合成。对它们的合成难易程度、理化性质以及在食蟹猴中的药代动力学参数进行比较后发现，3'-单-O-缬氨酰衍生物是所研究前药中最有前景的。该化合物正在作为一种新型抗乙肝病毒药物进行研发。
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