Orally bioavailable anti-HBV dinucleotide acyloxyalkyl prodrugs

Novel acyloxyalkyl dinucleotide prodrugs have been developed as orally bioavailable anti-HBV agents. 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 bioavailab...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-03, Vol.20 (5), p.1783-1786
Main Authors: Coughlin, John E., Padmanabhan, Seetharamaiyer, Zhang, Guangrong, Kirk, Cassandra J., Govardhan, Chandrika P., Korba, Brent E., O’Loughlin, Kathleen, Green, Carol E., Mirsalis, Jon, Morrey, John D., Iyer, Radhakrishnan P.
Format: Article
Language:English
Subjects:
ADME studies
Administration, Oral
Animals
Anti-HBV activity
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral activity
Antiviral agents
Antiviral Agents - chemical synthesis
Antiviral Agents - chemistry
Antiviral Agents - therapeutic use
Biological and medical sciences
Cell Line
Dinucleotide
Female
Hepatitis B - drug therapy
Hepatitis B virus
Hepatitis B virus - genetics
Humans
Male
Medical sciences
Mice
Mice, Transgenic
Mutation
Nucleotides - chemical synthesis
Nucleotides - chemistry
Nucleotides - therapeutic use
Oral bioavailability
Pharmacology. Drug treatments
Prodrugs
Prodrugs - chemical synthesis
Prodrugs - chemistry
Prodrugs - therapeutic use
Rats
Rats, Sprague-Dawley
Transgenic mouse model
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Description
Summary:Novel acyloxyalkyl dinucleotide prodrugs have been developed as orally bioavailable anti-HBV agents. 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).
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.01.010