Discovery of thienoimidazole-based HCV NS5A inhibitors. Part 1: C2-Symmetric inhibitors with diyne and biphenyl linkers

[Display omitted] The discovery of C2-symmetric bis-thienoimidazoles HCV NS5A inhibitors is herein reported. Two straightforward approaches to access the requisite diyne and biphenyl linker moieties are described. This study revealed the paramount importance of the aromatic character of the linker t...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2015-02, Vol.25 (4), p.936-939
Main Authors: Giroux, Simon, Bilimoria, Darius, Cadilhac, Caroline, Cottrell, Kevin M., Denis, Francois, Dietrich, Evelyne, Ewing, Nigel, Henderson, James A., L’Heureux, Lucille, Mani, Nagraj, Morris, Mark, Nicolas, Olivier, Reddy, T. Jagadeeswar, Selliah, Subajini, Shawgo, Rebecca S., Xu, Jinwang, Chauret, Nathalie, Berlioz-Seux, Francoise, Chan, Laval C., Das, Sanjoy K., Grillot, Anne-Laure, Bennani, Youssef L., Maxwell, John P.
Format: Article
Language:English
Subjects:
Antiviral Agents - chemistry
Antiviral Agents - pharmacology
Drug Discovery
HCV
Hepatitis C
Imidazoles - chemistry
Imidazoles - pharmacology
NS5a
Thienoimidazole
Viral Nonstructural Proteins - antagonists & inhibitors
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Summary:[Display omitted] The discovery of C2-symmetric bis-thienoimidazoles HCV NS5A inhibitors is herein reported. Two straightforward approaches to access the requisite diyne and biphenyl linker moieties are described. This study revealed the paramount importance of the aromatic character of the linker to achieve high genotype 1a potency.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2014.12.046