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Design, synthesis and anti-HBV activity of L-amino acid ester prodrugs of acyclic nucleoside phosphonates / 药学学报
Acta Pharmaceutica Sinica ; (12): 495-503, 2008.
Article in Chinese | WPRIM | ID: wpr-277824
ABSTRACT
To design and synthesis a series of novel L-amino acid esters prodrugs of acyclic nucleoside phosphonates with more potent anti-HBV activity, adefovir dipivoxil was used as lead compound, according to the results of enhanced oral bioavailability and antiviral activities of nucleoside L-amino acid ester prodrugs. Eleven novel L-amino acid ester prodrugs of acyclic nucleoside phosphonates were designed and synthesized, their anti-HBV activities were evaluated in HepG2 2.2.15 cells. Eight compounds exhibited antiviral activity, and compound 11 showed the most potent anti-HBV activity and highest selective index in vitro (EC50 0.0952 micromol x L(-1), SI 69523). Moreover, by analyzing the primary structure and activity relationship of these compounds, it could be suggested that L-amino acid ester strategy has significant potential in the acyclic nucleoside phosphonates prodrug design.
Subject(s)
Full text: Available Index: WPRIM (Western Pacific) Main subject: Antiviral Agents / Pathology / Pharmacology / Virology / Prodrugs / Chemistry / Hepatitis B virus / Cell Line, Tumor / Organophosphonates / Amino Acids Limits: Humans Language: Chinese Journal: Acta Pharmaceutica Sinica Year: 2008 Type: Article

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Full text: Available Index: WPRIM (Western Pacific) Main subject: Antiviral Agents / Pathology / Pharmacology / Virology / Prodrugs / Chemistry / Hepatitis B virus / Cell Line, Tumor / Organophosphonates / Amino Acids Limits: Humans Language: Chinese Journal: Acta Pharmaceutica Sinica Year: 2008 Type: Article