Discovery of thienoimidazole-based HCV NS5A inhibitors. Part 2: Non-symmetric inhibitors with potent activity against genotype 1a and 1b

[Display omitted] The discovery of non-symmetric thienoimidazole-containing HCV NS5A inhibitors is described. The inhibitors herein reported display high potencies against both genotype 1a and 1b. In this follow-up manuscript, we discuss the importance of the linker aromaticity to achieve high poten...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2015-02, Vol.25 (4), p.940-943
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:
Animals
Antiviral Agents - chemistry
Antiviral Agents - pharmacology
Genotype
HCV
Hepacivirus - drug effects
Hepacivirus - genetics
Hepatitis C
Hepatitis C virus
Humans
Imidazoles - chemistry
Imidazoles - pharmacology
NS5A
Rats
Thienoimidazole
Viral Nonstructural Proteins - drug effects
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Description
Summary:[Display omitted] The discovery of non-symmetric thienoimidazole-containing HCV NS5A inhibitors is described. The inhibitors herein reported display high potencies against both genotype 1a and 1b. In this follow-up manuscript, we discuss the importance of the linker aromaticity to achieve high potency, particularly against genotype 1a.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2014.12.044