Antiviral L-nucleosides specific for hepatitis B virus infection.
Antimicrob Agents Chemother
; 45(1): 229-35, 2001 Jan.
Article
em En
| MEDLINE
| ID: mdl-11120971
ABSTRACT
A unique series of simple "unnatural" nucleosides has been discovered to inhibit hepatitis B virus (HBV) replication. Through structure-activity analysis it was found that the 3'-OH group of the beta-L-2'-deoxyribose of the beta-L-2'-deoxynucleoside confers specific antihepadnavirus activity. The unsubstituted nucleosides beta-L-2'-deoxycytidine, beta-L-thymidine, and beta-L-2'-deoxyadenosine had the most potent, selective, and specific antiviral activity against HBV replication. Human DNA polymerases (alpha, beta, and gamma) and mitochondrial function were not affected. In the woodchuck model of chronic HBV infection, viral load was reduced by as much as 10(8) genome equivalents/ml of serum and there was no drug-related toxicity. In addition, the decline in woodchuck hepatitis virus surface antigen paralleled the decrease in viral load. These investigational drugs, used alone or in combination, are expected to offer new therapeutic options for patients with chronic HBV infection.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Contexto em Saúde:
2_ODS3
Problema de saúde:
2_enfermedades_transmissibles
Assunto principal:
Antivirais
/
Vírus da Hepatite B
/
Hepatite B
/
Nucleosídeos
Limite:
Animals
/
Female
/
Humans
/
Male
Idioma:
En
Revista:
Antimicrob Agents Chemother
Ano de publicação:
2001
Tipo de documento:
Article
País de afiliação:
Estados Unidos