title: Design and synthesis of highly potent and selective human peroxisome proliferator-activated receptor alpha agonists.
abstract: A combination of benzoxazole, phenoxyalkyl side chain, and phenoxybutyric acids was identified as a highly potent and selective human peroxisome proliferator-activated receptor alpha (PPARalpha) agonist. The synthesis, structure-activity relationship (SAR) studies, and in vivo activities of the representative compounds are described.
authors.affiliation: Tokyo New Drug Research Laboratories 1, Pharmaceutical Division, Kowa Co., LTD, 2-17-43, Noguchicho, Higashimurayam, Tokyo 189-0022, Japan. y-yamazk@kowa.co.jp
authors.forename: Yukiyoshi
authors.initials: Y
authors.lastname: Yamazaki
authors.forename: Kazutoyo
authors.initials: K
authors.lastname: Abe
authors.forename: Tsutomu
authors.initials: T
authors.lastname: Toma
authors.forename: Masahiro
authors.initials: M
authors.lastname: Nishikawa
authors.forename: Hidefumi
authors.initials: H
authors.lastname: Ozawa
authors.forename: Ayumu
authors.initials: A
authors.lastname: Okuda
authors.forename: Takaaki
authors.initials: T
authors.lastname: Araki
authors.forename: Soichi
authors.initials: S
authors.lastname: Oda
authors.forename: Keisuke
authors.initials: K
authors.lastname: Inoue
authors.forename: Kimiyuki
authors.initials: K
authors.lastname: Shibuya
authors.forename: Bart
authors.initials: B
authors.lastname: Staels
authors.forename: Jean-Charles
authors.initials: JC
authors.lastname: Fruchart
mesh_terms: D000485:Allergens; D000818:Animals; D052179:Antigens, Plant; D015195:Drug Design; D006571:Heterocyclic Compounds / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D000960:Hypolipidemic Agents / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D008822:Mice, Transgenic; D015394:Molecular Structure; D047493:PPAR alpha / Q000819:agonists*; D010940:Plant Proteins; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
chemical_list: D000485:Allergens; D052179:Antigens, Plant; D006571:Heterocyclic Compounds; D000960:Hypolipidemic Agents; C095551:MALD1 protein, Malus domestica; D047493:PPAR alpha; D010940:Plant Proteins