Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.

Ulrich Abel,Thomas Schlüter,Andreas Schulz,Eva Hambruch,Christoph Steeneck,Martin Hornberger,Thomas Hoffmann,Sanja Perović-Ottstadt,Olaf Kinzel,Michael Burnet,Ulrich Deuschle,Claus Kremoser

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

To overcome the known liabilities of GW4064 a series of analogues were synthesized with increased potency in vitro and with superior lipid lowering effects in db/db mice compared to 6-ethyl-CDCA.

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关键词

Farnesoid X receptor,FXR agonist,GW4064,db/db mice,Metabolic syndrome

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