1,5-Benzodiazepine inhibitors of HCV NS5B polymerase.
Bioorg Med Chem Lett
; 19(9): 2492-6, 2009 May 01.
Article
em En
| MEDLINE
| ID: mdl-19342234
ABSTRACT
Optimization through parallel synthesis of a novel series of hepatitis C virus (HCV) NS5B polymerase inhibitors led to the identification of (R)-11-(4-benzyloxy-2-fluorophenyl)-6-hydroxy-3,3-dimethyl-10-(6-methylpyridine-2-carbonyl)-2,3,4,5,10,11-hexahydro-dibenzo[b,e][1,4]diazepin-1-one 11zc and (R)-11-(4-benzyloxy-2-fluorophenyl)-6-hydroxy-3,3-dimethyl-10-(2,5-dimethyloxazol-4-carbonyl)-2,3,4,5,10,11-hexahydro-dibenzo[b,e][1,4]diazepin-1-one 11zk as potent (replicon EC(50)=400nM and 270nM, respectively) and selective (CC(50)>20muM) inhibitors of HCV replication. These data warrant further lead-optimization efforts.
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Base de dados:
MEDLINE
Assunto principal:
Antivirais
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Benzodiazepinas
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Química Farmacêutica
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Proteínas não Estruturais Virais
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Hepacivirus
Idioma:
En
Ano de publicação:
2009
Tipo de documento:
Article