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. 2015 Feb 15;25(4):940-3.
doi: 10.1016/j.bmcl.2014.12.044. Epub 2014 Dec 29.

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

Simon Giroux  1 , Darius Bilimoria  2 , Caroline Cadilhac  2 , Kevin M Cottrell  3 , Francois Denis  2 , Evelyne Dietrich  2 , Nigel Ewing  3 , James A Henderson  3 , Lucille L'Heureux  2 , Nagraj Mani  3 , Mark Morris  3 , Olivier Nicolas  2 , T Jagadeeswar Reddy  2 , Subajini Selliah  2 , Rebecca S Shawgo  3 , Jinwang Xu  3 , Nathalie Chauret  2 , Francoise Berlioz-Seux  3 , Laval C Chan  2 , Sanjoy K Das  2 , Anne-Laure Grillot  3 , Youssef L Bennani  3 , John P Maxwell  3
Affiliations

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

Simon Giroux et al. Bioorg Med Chem Lett. .

Abstract

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.

Keywords: HCV; Hepatitis C; NS5A; Thienoimidazole.

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