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Identification of the first potent, selective and bioavailable PPARα antagonist.
Bravo, Yalda; Baccei, Christopher S; Broadhead, Alex; Bundey, Richard; Chen, Austin; Clark, Ryan; Correa, Lucia; Jacintho, Jason D; Lorrain, Daniel S; Messmer, Davorka; Stebbins, Karin; Prasit, Peppi; Stock, Nicholas.
Afiliación
  • Bravo Y; Inception Sciences, 5871 Oberlin Drive Suite 100, San Diego, CA 92121, USA. Electronic address: yaldabravo47@gmail.com.
  • Baccei CS; Inception Sciences, 5871 Oberlin Drive Suite 100, San Diego, CA 92121, USA.
  • Broadhead A; Inception Sciences, 5871 Oberlin Drive Suite 100, San Diego, CA 92121, USA.
  • Bundey R; Inception Sciences, 5871 Oberlin Drive Suite 100, San Diego, CA 92121, USA.
  • Chen A; Inception Sciences, 5871 Oberlin Drive Suite 100, San Diego, CA 92121, USA.
  • Clark R; Inception Sciences, 5871 Oberlin Drive Suite 100, San Diego, CA 92121, USA.
  • Correa L; Inception Sciences, 5871 Oberlin Drive Suite 100, San Diego, CA 92121, USA.
  • Jacintho JD; Inception Sciences, 5871 Oberlin Drive Suite 100, San Diego, CA 92121, USA.
  • Lorrain DS; Inception Sciences, 5871 Oberlin Drive Suite 100, San Diego, CA 92121, USA.
  • Messmer D; Inception Sciences, 5871 Oberlin Drive Suite 100, San Diego, CA 92121, USA.
  • Stebbins K; Inception Sciences, 5871 Oberlin Drive Suite 100, San Diego, CA 92121, USA.
  • Prasit P; Inception Sciences, 5871 Oberlin Drive Suite 100, San Diego, CA 92121, USA.
  • Stock N; Inception Sciences, 5871 Oberlin Drive Suite 100, San Diego, CA 92121, USA.
Bioorg Med Chem Lett ; 24(10): 2267-72, 2014 May 15.
Article en En | MEDLINE | ID: mdl-24745969
The discovery and SAR of a novel series of potent and selective PPARα antagonists are herein described. Exploration of replacements for the labile acyl sulfonamide linker led to a biaryl sulfonamide series of which compound 33 proved to be suitable for further profiling in vivo. Compound 33 demonstrated excellent potency, selectivity against other nuclear hormone receptors, and good pharmacokinetics in mouse.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Sulfonamidas / PPAR alfa Tipo de estudio: Diagnostic_studies Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
Añadir a Mi BVS
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Sulfonamidas / PPAR alfa Tipo de estudio: Diagnostic_studies Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article Pais de publicación: Reino Unido