Synthesis and Pharmacological Properties of Linear Poly(Ethylene Glycol)s Conjugated to Interferon α-2b by Azo Coupling

摘要

A method for the preparation of pharmacologically active conjugates of interferon α-2b with poly(ethylene glycol)s that absorbed in the visible spectral range was proposed. New covalent conjugates of linear poly(ethylene glycol)s with interferon α-2b were prepared via diazotization of 4-aminobenzoic acid poly(ethylene glycol) esters followed by azo coupling of the obtained diazonium salts with histidine imidazoles and tyrosine phenols of the protein amino-acid chain. The synthesized conjugates retained a high degree of interferon α-2b antiviral activity in vitro and had longer blood circulation times than a foreign analog and very low acute toxicity and immunogenicity.