Discovery of Thienoimidazole-Based HCV NS5A Genotype 1a and 1b Inhibitors.
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ABSTRACT:
SUBMITTER: Giroux S
PROVIDER: S-EPMC4027595 | biostudies-literature | 2014 Mar
REPOSITORIES: biostudies-literature
Publications
Discovery of Thienoimidazole-Based HCV NS5A Genotype 1a and 1b Inhibitors.
Giroux Simon S Xu Jinwang J Reddy T Jagadeeswar TJ Morris Mark M Cottrell Kevin M KM Cadilhac Caroline C Henderson James A JA Nicolas Oliver O Bilimoria Darius D Denis Francois F Mani Nagraj N Ewing Nigel N Shawgo Rebecca R L'Heureux Lucille L Selliah Subajini S Chan Laval L Chauret Nathalie N Berlioz-Seux Francoise F Namchuk Mark N MN Grillot Anne-Laure AL Bennani Youssef L YL Das Sanjoy K SK Maxwell John P JP
ACS medicinal chemistry letters 20130127 3
The discovery of potent thienoimidazole-based HCV NS5A inhibitors is herein reported. A novel method to access the thienoimidazole [5,5]-bicyclic system is disclosed. This method gave access to a common key intermediate (6) that was engaged in Suzuki or Sonogashira reactions with coupling partners bearing different linkers. A detailed study of the structure-activity relationship (SAR) of the linkers revealed that aromatic linkers with linear topologies are required to achieve high potency for bo ...[more]
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