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Discovery of thienoimidazole-based HCV NS5A inhibitors. Part 1: C2-symmetric inhibitors with diyne and biphenyl linkers.
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.
Afiliação
  • Giroux S; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, MA 02210, USA.
  • Bilimoria D; Vertex Pharmaceuticals Canada Inc., 275 Boul. Armand-Frappier, Laval, QC H7V 4A7, Canada.
  • Cadilhac C; Vertex Pharmaceuticals Canada Inc., 275 Boul. Armand-Frappier, Laval, QC H7V 4A7, Canada.
  • Cottrell KM; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, MA 02210, USA.
  • Denis F; Vertex Pharmaceuticals Canada Inc., 275 Boul. Armand-Frappier, Laval, QC H7V 4A7, Canada.
  • Dietrich E; Vertex Pharmaceuticals Canada Inc., 275 Boul. Armand-Frappier, Laval, QC H7V 4A7, Canada.
  • Ewing N; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, MA 02210, USA.
  • Henderson JA; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, MA 02210, USA.
  • L'Heureux L; Vertex Pharmaceuticals Canada Inc., 275 Boul. Armand-Frappier, Laval, QC H7V 4A7, Canada.
  • Mani N; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, MA 02210, USA.
  • Morris M; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, MA 02210, USA.
  • Nicolas O; Vertex Pharmaceuticals Canada Inc., 275 Boul. Armand-Frappier, Laval, QC H7V 4A7, Canada.
  • Reddy TJ; Vertex Pharmaceuticals Canada Inc., 275 Boul. Armand-Frappier, Laval, QC H7V 4A7, Canada.
  • Selliah S; Vertex Pharmaceuticals Canada Inc., 275 Boul. Armand-Frappier, Laval, QC H7V 4A7, Canada.
  • Shawgo RS; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, MA 02210, USA.
  • Xu J; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, MA 02210, USA.
  • Chauret N; Vertex Pharmaceuticals Canada Inc., 275 Boul. Armand-Frappier, Laval, QC H7V 4A7, Canada.
  • Berlioz-Seux F; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, MA 02210, USA.
  • Chan LC; Vertex Pharmaceuticals Canada Inc., 275 Boul. Armand-Frappier, Laval, QC H7V 4A7, Canada.
  • Das SK; Vertex Pharmaceuticals Canada Inc., 275 Boul. Armand-Frappier, Laval, QC H7V 4A7, Canada.
  • Grillot AL; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, MA 02210, USA.
  • Bennani YL; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, MA 02210, USA.
  • Maxwell JP; Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, MA 02210, USA.
Bioorg Med Chem Lett ; 25(4): 936-9, 2015 Feb 15.
Article em En | MEDLINE | ID: mdl-25595681
ABSTRACT
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.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Antivirais / Proteínas não Estruturais Virais / Descoberta de Drogas / Imidazóis Idioma: En Ano de publicação: 2015 Tipo de documento: Article
Texto completo
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XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Antivirais / Proteínas não Estruturais Virais / Descoberta de Drogas / Imidazóis Idioma: En Ano de publicação: 2015 Tipo de documento: Article