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2-Alkyloxazoles as potent and selective PI4KIIIß inhibitors demonstrating inhibition of HCV replication.
Keaney, Erin P; Connolly, Michael; Dobler, Markus; Karki, Rajeshri; Honda, Ayako; Sokup, Samantha; Karur, Subramanian; Britt, Shawn; Patnaik, Anup; Raman, Prakash; Hamann, Lawrence G; Wiedmann, Brigitte; LaMarche, Matthew J.
Afiliación
  • Keaney EP; Global Discovery Chemistry, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, USA. Electronic address: erin.keaney@novartis.com.
  • Connolly M; Global Discovery Chemistry, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, USA.
  • Dobler M; Global Discovery Chemistry, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, USA.
  • Karki R; Global Discovery Chemistry, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, USA.
  • Honda A; Global Discovery Chemistry, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, USA.
  • Sokup S; Global Discovery Chemistry, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, USA.
  • Karur S; Global Discovery Chemistry, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, USA.
  • Britt S; Global Discovery Chemistry, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, USA.
  • Patnaik A; Global Discovery Chemistry, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, USA.
  • Raman P; Global Discovery Chemistry, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, USA.
  • Hamann LG; Global Discovery Chemistry, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, USA.
  • Wiedmann B; Infectious Disease Area, Novartis Institutes for Biomedical Research, 100 Technology Square, Cambridge, MA 02139, USA.
  • LaMarche MJ; Global Discovery Chemistry, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, USA.
Bioorg Med Chem Lett ; 24(16): 3714-8, 2014 Aug 15.
Article en En | MEDLINE | ID: mdl-25065492
ABSTRACT
Synthesis and SAR of 2-alkyloxazoles as class III phosphatidylinositol-4-kinase beta (PI4KIIIß) inhibitors is described. These compounds demonstrate that inhibition of PI4KIIIß leads to potent inhibition of HCV replication as observed in genotype (GT) 1a and 1b replicon and GT2a JFH1 virus assays in vitro.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antivirales / Oxazoles / Replicación Viral / Fosfotransferasas (Aceptor de Grupo Alcohol) / Hepacivirus / Inhibidores de Proteínas Quinasas Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antivirales / Oxazoles / Replicación Viral / Fosfotransferasas (Aceptor de Grupo Alcohol) / Hepacivirus / Inhibidores de Proteínas Quinasas Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article