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Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine.
Koltun, Dmitry O; Parkhill, Eric Q; Elzein, Elfatih; Kobayashi, Tetsuya; Notte, Gregory T; Kalla, Rao; Jiang, Robert H; Li, Xiaofen; Perry, Thao D; Avila, Belem; Wang, Wei-Qun; Smith-Maxwell, Catherine; Dhalla, Arvinder K; Rajamani, Sridharan; Stafford, Brian; Tang, Jennifer; Mollova, Nevena; Belardinelli, Luiz; Zablocki, Jeff A.
Afiliación
  • Koltun DO; Department of Medicinal Chemistry, Gilead Sciences Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Parkhill EQ; Department of Medicinal Chemistry, Gilead Sciences Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Elzein E; Department of Medicinal Chemistry, Gilead Sciences Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Kobayashi T; Department of Medicinal Chemistry, Gilead Sciences Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Notte GT; Department of Medicinal Chemistry, Gilead Sciences Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Kalla R; Department of Medicinal Chemistry, Gilead Sciences Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Jiang RH; Department of Medicinal Chemistry, Gilead Sciences Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Li X; Department of Medicinal Chemistry, Gilead Sciences Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Perry TD; Department of Medicinal Chemistry, Gilead Sciences Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Avila B; Department of Medicinal Chemistry, Gilead Sciences Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Wang WQ; Department of Biological Sciences, Gilead Sciences Inc., 333, Fremont, CA 94555, USA.
  • Smith-Maxwell C; Department of Biological Sciences, Gilead Sciences Inc., 333, Fremont, CA 94555, USA.
  • Dhalla AK; Department of Biological Sciences, Gilead Sciences Inc., 333, Fremont, CA 94555, USA.
  • Rajamani S; Department of Biological Sciences, Gilead Sciences Inc., 333, Fremont, CA 94555, USA.
  • Stafford B; Department of Drug Metabolism, Gilead Sciences Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Tang J; Department of Drug Metabolism, Gilead Sciences Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Mollova N; Department of Drug Metabolism, Gilead Sciences Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Belardinelli L; Department of Biological Sciences, Gilead Sciences Inc., 333, Fremont, CA 94555, USA.
  • Zablocki JA; Department of Medicinal Chemistry, Gilead Sciences Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
Bioorg Med Chem Lett ; 26(13): 3202-3206, 2016 07 01.
Article en En | MEDLINE | ID: mdl-27080178
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Piridinas / Triazoles / Bloqueadores de los Canales de Sodio / Descubrimiento de Drogas / Canal de Sodio Activado por Voltaje NAV1.5 / Ranolazina / Corazón Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2016 Tipo del documento: Article País de afiliación: Estados Unidos
Texto completo
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Piridinas / Triazoles / Bloqueadores de los Canales de Sodio / Descubrimiento de Drogas / Canal de Sodio Activado por Voltaje NAV1.5 / Ranolazina / Corazón Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2016 Tipo del documento: Article País de afiliación: Estados Unidos