Chemical modified adefovir and tynofovir

Abstract

A chemically modified adefovir and tenofovir is prepared through the combination of adefovir (or tenofovir) with polyethanediol (or glycosylated polyethanediol). Their preparing process and their antiviral application are also disclosed.

Description

Chemically modified adefovir or tenofovir technical field The present invention relates to the chemical modification of drug molecules to improve the deficiencies of existing drugs, specifically the combination of Adefovir (Adefovir, PMEA) or tenofovir (tenofovir, PMPA) and polyethylene glycol, Adefovir (PMEA) The combination of defovir or tenofovir and glycosylated polyethylene glycol also relates to their preparation method and antiviral application. Background technique Adefovir and Tenofovir are nucleoside analogues with similar structures and have broad-spectrum antiviral activity. Their structural formulas are: Among them, A can choose H or CH3. When A represents H, it is adefovir; when A represents CH3, it is tenofovir. Clinical trials have found that both adefovir and tenofovir have good anti-AIDS virus (HIV) and hepatitis B virus (HBV) activities. Experiments have confirmed that adefovir and tenofovir have significant inhibitory effects on the replication an...

AI Technical Summary

Problems solved by technology

Since the core antigen of hepatitis B virus exists in the liver cells, nucleoside drugs need to enter the liver cells and be effective after phosphorylation catalyzed by thymidine kinase. The cells lack thymidine kinase, the phosphorylation of host cells is slow, and the effective concentration for inhibiting virus replication cannot be reached. Large doses of drugs can increase the blood drug concentration, but the drug that has not been phosphorylated in the blood can quickly pass through the kidneys. Toxic side effects such as hematuria and renal dysfunction due to excretion (WorldChinJDigestol2003June; 11(6):799-802)

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