2. Academic Validation
  3. Novel heterocyclic scaffolds of GW4064 as farnesoid X receptor agonists

Novel heterocyclic scaffolds of GW4064 as farnesoid X receptor agonists

  • Bioorg Med Chem Lett. 2015 Jan 15;25(2):280-4. doi: 10.1016/j.bmcl.2014.11.050.
Terrence L Smalley Jr 1,  Sharon Boggs 2,  Justin A Caravella 3,  Lihong Chen 4,  Katrina L Creech 5,  David N Deaton 2,  Istvan Kaldor 2,  Derek J Parks 5
Affiliations

Affiliations

  • 1 Muscle Metabolism DPU, Metabolic Pathways & Cardiovascular Discovery Performance Unit, GlaxoSmithKline, Inc., Five Moore Drive, Research Triangle Park, NC 27709, United States. Electronic address: terry.l.smalley@gsk.com.
  • 2 Muscle Metabolism DPU, Metabolic Pathways & Cardiovascular Discovery Performance Unit, GlaxoSmithKline, Inc., Five Moore Drive, Research Triangle Park, NC 27709, United States.
  • 3 Computational and Structural Sciences, Platform Technology & Science, GlaxoSmithKline, Inc., Five Moore Drive, Research Triangle Park, NC 27709, United States.
  • 4 Enteroendocrine DPU, Metabolic Pathways & Cardiovascular Discovery Performance Unit, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, United States.
  • 5 Molecular Discovery Research, Platform Technology & Science, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, United States.
PMID: 25499883 DOI: 10.1016/j.bmcl.2014.11.050
Abstract

The farnesoid X receptor (FXR) may play a crucial role in a number of metabolic diseases and, as such, could potentially serve as a target for the development of therapeutics as a treatment for those diseases. Previous work has described GW4064 as an FXR Agonist with an interesting activity profile. This manuscript will describe the synthesis of novel analogs of GW4064 and the activity profile of those analogs.

Keywords

FXR agonist; Heterocycles; Liver.

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