Your browser doesn't support javascript.
loading
Synthesis and characterization of a series of chiral alkoxymethyl morpholine analogs as dopamine receptor 4 (D4R) antagonists.
Witt, Jonathan O; McCollum, Andrea L; Hurtado, Miguel A; Huseman, Eric D; Jeffries, Daniel E; Temple, Kayla J; Plumley, Hyekyung C; Blobaum, Anna L; Lindsley, Craig W; Hopkins, Corey R.
Afiliación
  • Witt JO; Department of Chemistry, Vanderbilt University, Nashville, TN 37232, United States.
  • McCollum AL; Department of Chemistry, Vanderbilt University, Nashville, TN 37232, United States.
  • Hurtado MA; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States.
  • Huseman ED; Department of Chemistry, Vanderbilt University, Nashville, TN 37232, United States.
  • Jeffries DE; Department of Chemistry, Vanderbilt University, Nashville, TN 37232, United States.
  • Temple KJ; Department of Chemistry, Vanderbilt University, Nashville, TN 37232, United States.
  • Plumley HC; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, United States.
  • Blobaum AL; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, United States.
  • Lindsley CW; Department of Chemistry, Vanderbilt University, Nashville, TN 37232, United States; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, Unit
  • Hopkins CR; Department of Chemistry, Vanderbilt University, Nashville, TN 37232, United States; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, Unit
Bioorg Med Chem Lett ; 26(10): 2481-2488, 2016 05 15.
Article en En | MEDLINE | ID: mdl-27080176
Herein, we report the synthesis and structure-activity relationship of a series of chiral alkoxymethyl morpholine analogs. Our efforts have culminated in the identification of (S)-2-(((6-chloropyridin-2-yl)oxy)methyl)-4-((6-fluoro-1H-indol-3-yl)methyl)morpholine as a novel potent and selective dopamine D4 receptor antagonist with selectivity against the other dopamine receptors tested (<10% inhibition at 1µM against D1, D2L, D2S, D3, and D5).
Asunto(s)
Palabras clave
Texto completo
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Relación Estructura-Actividad / Morfolinas / Antagonistas de Dopamina / Receptores de Dopamina D4 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: Relación Estructura-Actividad / Morfolinas / Antagonistas de Dopamina / Receptores de Dopamina D4 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