2. Academic Validation
  3. FXR agonist activity of conformationally constrained analogs of GW 4064

FXR agonist activity of conformationally constrained analogs of GW 4064

  • Bioorg Med Chem Lett. 2009 Aug 15;19(16):4733-9. doi: 10.1016/j.bmcl.2009.06.062.
Adwoa Akwabi-Ameyaw 1,  Jonathan Y Bass,  Richard D Caldwell,  Justin A Caravella,  Lihong Chen,  Katrina L Creech,  David N Deaton,  Kevin P Madauss,  Harry B Marr,  Robert B McFadyen,  Aaron B Miller,  Frank Navas 3rd,  Derek J Parks,  Paul K Spearing,  Dan Todd,  Shawn P Williams,  G Bruce Wisely
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA.
PMID: 19586769 DOI: 10.1016/j.bmcl.2009.06.062
Abstract

Two series of conformationally constrained analogs of the FXR Agonist GW 4064 1 were prepared. Replacement of the metabolically labile stilbene with either benzothiophene or naphthalene rings led to the identification of potent full agonists 2a and 2g.

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