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Conformationally constrained farnesoid X receptor (FXR) agonists: alternative replacements of the stilbene |
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| Authors: | Akwabi-Ameyaw Adwoa Caravella Justin A Chen Lihong Creech Katrina L Deaton David N Madauss Kevin P Marr Harry B Miller Aaron B Navas Frank Parks Derek J Spearing Paul K Todd Dan Williams Shawn P Wisely G Bruce |
| Institution: | Department of Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA. |
| 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. |
| Keywords: | Farnesoid X receptor FXR Nuclear receptor modulator FXR X-ray co-crystal structure GW 4064 GSK8062 GSK2324 Bile acid receptor NR1H4 |
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