title: FXR agonist activity of conformationally constrained analogs of GW 4064.
abstract: Two series of conformationally constrained analogs of the FXR agonist GW 4064 1 were prepared. Replacement of the metabolically labile stilbene with either benzothiophene or naphthalene rings led to the identification of potent full agonists 2a and 2g.
authors: Department of Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA.
authors: Adwoa
authors: A
authors: Akwabi-Ameyaw
authors: Jonathan Y
authors: JY
authors: Bass
authors: Richard D
authors: RD
authors: Caldwell
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: Robert B
authors: RB
authors: McFadyen
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
authors: G
authors: Bruce Wisely
mesh_terms: D000818:Animals; D001665:Binding Sites; D003198:Computer Simulation; D018360:Crystallography, X-Ray; D006801:Humans; D007555:Isoxazoles / Q000737:chemistry* / Q000494:pharmacology; D009281:Naphthalenes / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000737:chemistry* / Q000493:pharmacokinetics; D000099150:Receptor, Farnesoid X-Activated
chemical_list: D007555:Isoxazoles; D009281:Naphthalenes; D018160:Receptors, Cytoplasmic and Nuclear; D013876:Thiophenes; D000099150:Receptor, Farnesoid X-Activated; C412815:GW 4064