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

Adwoa Akwabi-Ameyaw,Justin A Caravella,Lihong Chen,Katrina L Creech,David N Deaton,Kevin P Madauss,Harry B Marr,Aaron B Miller,Frank Navas,Derek J Parks,Paul K Spearing,Dan Todd,Shawn P Williams,G Bruce Wisely

Bioorganic & Medicinal Chemistry Letters（2011）

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摘要

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 benzothiophene1f and the indole 1g display the optimal orientation of the carboxylate for enhanced FXR agonist potency.

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关键词

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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