title: Coupling of antiviral nucleoside analogs to lactosaminated human albumin by using the imidazolides of their phosphoric esters.
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.
authors.affiliation: Department of Experimental Pathology, University of Bologna, Italy.
authors.forename: L
authors.initials: L
authors.lastname: Fiume
authors.forename: C
authors.initials: C
authors.lastname: Busi
authors.forename: G
authors.initials: G
authors.lastname: Di Stefano
authors.forename: A
authors.initials: A
authors.lastname: Mattioli
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers; D004355:Drug Stability; D004591:Electrophoresis, Polyacrylamide Gel; D004952:Esters / Q000138:chemical synthesis; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007093:Imidazoles / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D007526:Isoelectric Point; D008099:Liver / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D009705:Nucleosides / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D010756:Phosphoric Acids / Q000138:chemical synthesis; D010758:Phosphorus; D051381:Rats; D012709:Serum Albumin / Q000138:chemical synthesis* / Q000494:pharmacology; D001084:Vidarabine Phosphate / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D000998:Antiviral Agents; D004337:Drug Carriers; D004952:Esters; D007093:Imidazoles; D009705:Nucleosides; D010756:Phosphoric Acids; D012709:Serum Albumin; C046912:lactosaminated serum albumin; D001084:Vidarabine Phosphate; D010758:Phosphorus