title: Conformationally constrained farnesoid X receptor (FXR) agonists: alternative replacements of the stilbene.
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.
authors: Department of Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA.
authors: Adwoa
authors: A
authors: Akwabi-Ameyaw
authors: Justin A
authors: JA
authors: Caravella
authors: Lihong
authors: L
authors: Chen
authors: Katrina L
authors: KL
authors: Creech
authors: David N
authors: DN
authors: Deaton
authors: Kevin P
authors: KP
authors: Madauss
authors: Harry B
authors: HB
authors: Marr
authors: Aaron B
authors: AB
authors: Miller
authors: Frank
authors: F
authors: Navas
authors: Derek J
authors: DJ
authors: Parks
authors: Paul K
authors: PK
authors: Spearing
authors: Dan
authors: D
authors: Todd
authors: Shawn P
authors: SP
authors: Williams
authors: G Bruce
authors: GB
authors: Wisely
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D002460:Cell Line; D006801:Humans; D007555:Isoxazoles / Q000737:chemistry* / Q000494:pharmacology*; D008968:Molecular Conformation; D008969:Molecular Sequence Data; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists* / Q000378:metabolism; D013267:Stilbenes / Q000737:chemistry* / Q000494:pharmacology*; D000099150:Receptor, Farnesoid X-Activated
chemical_list: D007555:Isoxazoles; D018160:Receptors, Cytoplasmic and Nuclear; D013267:Stilbenes; D000099150:Receptor, Farnesoid X-Activated; C412815:GW 4064