1.
Bioorg Med Chem Lett
; 20(5): 1783-6, 2010 Mar 01.
Article
in English
| MEDLINE
| ID: mdl-20117930
ABSTRACT
The acyloxyalkyl derivatives of a model anti-HBV dinucleotide were synthesized and evaluated as orally bioavailable prodrugs. Our studies have led to the identification of the first orally bioavailable dinucleotide prodrugs for further therapeutic development against the hepatitis B virus (HBV).
Subject(s)
Antiviral Agents/chemistry , Hepatitis B virus/genetics , Hepatitis B/drug therapy , Nucleotides/chemistry , Prodrugs/chemistry , Administration, Oral , Animals , Antiviral Agents/chemical synthesis , Antiviral Agents/therapeutic use , Cell Line , Female , Humans , Male , Mice , Mice, Transgenic , Mutation , Nucleotides/chemical synthesis , Nucleotides/therapeutic use , Prodrugs/chemical synthesis , Prodrugs/therapeutic use , Rats , Rats, Sprague-Dawley
2.
Bioorg Med Chem Lett
; 16(6): 1491-4, 2006 Mar 15.
Article
in English
| MEDLINE
| ID: mdl-16387496
ABSTRACT
Several pronucleotide analogs of the model anti-HBV dinucleotide 3'-dA-U(2'OMe) have been synthesized and evaluated for stability, bioreversibility and cytotoxicity. These studies have helped identify potential candidates for further evaluation.
