title: Identification of a series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids with activity on PPARalpha, PPARgamma, and PPARdelta.
abstract: A series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids with dual agonist activity on PPARalpha and PPARgamma is described. Several of these compounds also showed partial agonist activity on PPARdelta. Resolution of one analogue showed that PPARalpha and PPARgamma activity resided in mainly one enantiomer, whereas PPARdelta activity was retained in both enantiomers.
authors.affiliation: Nuclear Receptor Discovery Research, GlaxoSmithKline, Research Triangle Park, NC 27709, USA. kevin_liu@stromix.com
authors.forename: K G
authors.initials: KG
authors.lastname: Liu
authors.forename: J S
authors.initials: JS
authors.lastname: Smith
authors.forename: A H
authors.initials: AH
authors.lastname: Ayscue
authors.forename: B R
authors.initials: BR
authors.lastname: Henke
authors.forename: M H
authors.initials: MH
authors.lastname: Lambert
authors.forename: L M
authors.initials: LM
authors.lastname: Leesnitzer
authors.forename: K D
authors.initials: KD
authors.lastname: Plunket
authors.forename: T M
authors.initials: TM
authors.lastname: Willson
authors.forename: D D
authors.initials: DD
authors.lastname: Sternbach
mesh_terms: D002851:Chromatography, High Pressure Liquid; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007536:Isomerism; D010069:Oxadiazoles / Q000737:chemistry; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists*; D013329:Structure-Activity Relationship; D014157:Transcription Factors / Q000819:agonists*
chemical_list: D010069:Oxadiazoles; D018160:Receptors, Cytoplasmic and Nuclear; D014157:Transcription Factors