Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2009 May 1;19(9):2492-6.
doi: 10.1016/j.bmcl.2009.03.035. Epub 2009 Mar 14.

1,5-Benzodiazepine inhibitors of HCV NS5B polymerase

David McGowan  1 , Origène Nyanguile, Maxwell D Cummings, Sandrine Vendeville, Koen Vandyck, Walter Van den Broeck, Carlo W Boutton, Hendrik De Bondt, Ludo Quirynen, Katie Amssoms, Jean-François Bonfanti, Stefaan Last, Klara Rombauts, Abdellah Tahri, Lili Hu, Frédéric Delouvroy, Katrien Vermeiren, Geneviève Vandercruyssen, Liesbet Van der Helm, Erna Cleiren, Wendy Mostmans, Pedro Lory, Geert Pille, Kristof Van Emelen, Gregory Fanning, Frederik Pauwels, Tse-I Lin, Kenneth Simmen, Pierre Raboisson
Affiliations

1,5-Benzodiazepine inhibitors of HCV NS5B polymerase

David McGowan et al. Bioorg Med Chem Lett. .

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.

PubMed Disclaimer

MeSH terms

LinkOut - more resources