title: Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.
abstract: Propionic acid derivative 8, which was designed and synthesized based on putative pharmacophores of known PPARgamma- and PPARalpha-selective compounds, exhibits potent dual PPARalpha/gamma agonist activity as demonstrated by in vitro binding and dose overlap in the newly introduced EOB mouse model for glucose lowering and lipid/cholesterol homeostasis.
authors.affiliation: Lilly Research Laboratories, A Division of Eli Lilly & Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA. Brooks_Dawn_A@Lilly.com
authors.forename: D A
authors.initials: DA
authors.lastname: Brooks
authors.forename: G J
authors.initials: GJ
authors.lastname: Etgen
authors.forename: C J
authors.initials: CJ
authors.lastname: Rito
authors.forename: A J
authors.initials: AJ
authors.lastname: Shuker
authors.forename: S J
authors.initials: SJ
authors.lastname: Dominianni
authors.forename: A M
authors.initials: AM
authors.lastname: Warshawsky
authors.forename: R
authors.initials: R
authors.lastname: Ardecky
authors.forename: J R
authors.initials: JR
authors.lastname: Paterniti
authors.forename: J
authors.initials: J
authors.lastname: Tyhonas
authors.forename: D S
authors.initials: DS
authors.lastname: Karanewsky
authors.forename: R F
authors.initials: RF
authors.lastname: Kauffman
authors.forename: C L
authors.initials: CL
authors.lastname: Broderick
authors.forename: B A
authors.initials: BA
authors.lastname: Oldham
authors.forename: C
authors.initials: C
authors.lastname: Montrose-Rafizadeh
authors.forename: L L
authors.initials: LL
authors.lastname: Winneroski
authors.forename: M M
authors.initials: MM
authors.lastname: Faul
authors.forename: J R
authors.initials: JR
authors.lastname: McCarthy
mesh_terms: D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D008076:Cholesterol, HDL / Q000097:blood; D003920:Diabetes Mellitus / Q000097:blood / Q000188:drug therapy / Q000235:genetics; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D015195:Drug Design; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D051379:Mice; D008815:Mice, Inbred Strains; D011422:Propionates / Q000138:chemical synthesis* / Q000494:pharmacology*; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists* / Q000235:genetics; D014157:Transcription Factors / Q000819:agonists* / Q000235:genetics; D014280:Triglycerides / Q000097:blood
chemical_list: D001786:Blood Glucose; D008076:Cholesterol, HDL; D007004:Hypoglycemic Agents; D011422:Propionates; D018160:Receptors, Cytoplasmic and Nuclear; D014157:Transcription Factors; D014280:Triglycerides