2. Academic Validation
  3. Conformationally constrained farnesoid X receptor (FXR) agonists: alternative replacements of the stilbene

Conformationally constrained farnesoid X receptor (FXR) agonists: alternative replacements of the stilbene

  • Bioorg Med Chem Lett. 2011 Oct 15;21(20):6154-60. doi: 10.1016/j.bmcl.2011.08.034.
Adwoa Akwabi-Ameyaw 1,  Justin A Caravella,  Lihong Chen,  Katrina L Creech,  David N Deaton,  Kevin P Madauss,  Harry B Marr,  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: 21890356 DOI: 10.1016/j.bmcl.2011.08.034
Abstract

To further explore the optimum placement of the acid moiety in conformationally constrained analogs of GW 4064 1a, a series of stilbene replacements were prepared. The benzothiophene 1f and the indole 1g display the optimal orientation of the carboxylate for enhanced FXR Agonist potency.

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