| Literature DB >> 19342234 |
David McGowan1, 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.
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.Entities:
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Year: 2009 PMID： 19342234 DOI： 10.1016/j.bmcl.2009.03.035
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823