Abstract
Liver targeting of antiviral nucleoside analogs can be obtained by conjugating these drugs with the hepatotropic molecule lactosaminated serum albumin. We describe a new coupling procedure which uses the imidazolides of the phosphoric ester derivatives of the drugs in an alkaline medium. By this procedure conjugates are obtained with a high drug/carrier molar ratio and without the unwanted protein chemical changes produced by carbodiimides usually employed for this coupling.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antiviral Agents / chemical synthesis*
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Antiviral Agents / pharmacokinetics
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Antiviral Agents / pharmacology
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Chemistry, Pharmaceutical
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Drug Carriers
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Drug Stability
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Electrophoresis, Polyacrylamide Gel
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Esters / chemical synthesis
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Humans
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Hydrogen-Ion Concentration
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Imidazoles / chemical synthesis*
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Imidazoles / pharmacokinetics
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Imidazoles / pharmacology
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Isoelectric Point
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Liver / metabolism
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Magnetic Resonance Spectroscopy
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Nucleosides / chemical synthesis*
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Nucleosides / pharmacokinetics
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Nucleosides / pharmacology
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Phosphoric Acids / chemical synthesis
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Phosphorus
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Rats
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Serum Albumin / chemical synthesis*
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Serum Albumin / pharmacology
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Vidarabine Phosphate / chemical synthesis
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Vidarabine Phosphate / pharmacokinetics
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Vidarabine Phosphate / pharmacology
Substances
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Antiviral Agents
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Drug Carriers
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Esters
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Imidazoles
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Nucleosides
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Phosphoric Acids
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Serum Albumin
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lactosaminated serum albumin
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Vidarabine Phosphate
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Phosphorus