A Comprehensive Insight into the Chemical Space and ADME Features of Small Molecule NS5A Inhibitors.
Curr Top Med Chem
; 16(12): 1372-82, 2016.
Article
em En
| MEDLINE
| ID: mdl-26585933
ABSTRACT
Non-structural 5A (NS5A) protein plays a crucial role in the replication of hepatitis C virus (HCV) and during the past decade has attracted increasing attention as a promising biological target for the treatment of viral infections and related disorders. Small-molecule NS5A inhibitors have shown significant antiviral activity in vitro and in vivo. Several lead molecules are reasonably regarded as novel highly potent drug candidates with favorable ADME features and tolerable side effects. The first-in-class daclatasvir has recently been launched into the market and 14 novel molecules are currently under evaluation in clinical trials. From this perspective, we provide an overview of the available chemical space of small-molecule NS5A inhibitors and their PK properties, mainly focusing on the diversity in structure and scaffold representation.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Antivirais
/
Proteínas não Estruturais Virais
/
Hepacivirus
/
Bibliotecas de Moléculas Pequenas
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Curr Top Med Chem
Assunto da revista:
QUIMICA
Ano de publicação:
2016
Tipo de documento:
Article
País de afiliação:
Federação Russa