Study on 2-arylthio-5-iodo pyrimidine derivatives as novel nonnucleoside inhibitors against hepatitis B virus DNA replication.
Future Med Chem
; 8(7): 751-63, 2016 05.
Article
em En
| MEDLINE
| ID: mdl-27172826
ABSTRACT
BACKGROUND:
Novel nonnucleoside hepatitis B virus inhibitors have been recently developed for the reason of drug-resistant mutations and adverse effects of nucleoside analogs. In this study, two series of 2-arylthio-5-iodo pyrimidine analogs were firstly reported as potential anti-HBV agents.METHODOLOGY:
Target compounds were prepared according to two high-yielded synthetic routes, and their anti-HBV activities were evaluated on Hep2.2.15 and HepAD38 cell lines, respectively. To probe the mechanism of active agents, a cell-based (Huh-7) study of biochemical markers (e.g., HBeAg, HBsAg, intracellular HBV DNA and pgRNA) was performed. Furthermore, the pharmacophore models were constructed for future optimization of lead compounds.CONCLUSION:
2-Arylthio-5-iodo pyrimidine derivatives firstly proved to be effective against HBV, which paves the way for future development of nonnucleoside anti-HBV agents.Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Contexto em Saúde:
2_ODS3
Problema de saúde:
2_enfermedades_transmissibles
Assunto principal:
Antivirais
/
Pirimidinas
/
Sulfetos
/
DNA Viral
/
Vírus da Hepatite B
/
Replicação do DNA
Limite:
Humans
Idioma:
En
Revista:
Future Med Chem
Ano de publicação:
2016
Tipo de documento:
Article
País de afiliação:
China