Discovery of Ruzasvir (MK-8408): A Potent, Pan-Genotype HCV NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Polymorphisms.
J Med Chem
; 60(1): 290-306, 2017 01 12.
Article
em En
| MEDLINE
| ID: mdl-27808515
ABSTRACT
We describe the research that led to the discovery of compound 40 (ruzasvir, MK-8408), a pan-genotypic HCV nonstructural protein 5A (NS5A) inhibitor with a "flat" GT1 mutant profile. This NS5A inhibitor contains a unique tetracyclic indole core while maintaining the imidazole-proline-valine Moc motifs of our previous NS5A inhibitors. Compound 40 is currently in early clinical trials and is under evaluation as part of an all-oral DAA regimen for the treatment of chronic HCV infection.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Antivirais
/
Polimorfismo Genético
/
Pirrolidinas
/
Tiazóis
/
Proteínas não Estruturais Virais
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Hepacivirus
/
Compostos Heterocíclicos de 4 ou mais Anéis
Tipo de estudo:
Risk_factors_studies
Limite:
Animals
/
Humans
Idioma:
En
Revista:
J Med Chem
Assunto da revista:
QUIMICA
Ano de publicação:
2017
Tipo de documento:
Article