title: Design, synthesis and evaluation of substituted phenylpropanoic acid derivatives as peroxisome proliferator-activated receptor (PPAR) activators: novel human PPARalpha-selective activators.
abstract: A series of substituted phenylpropanoic acid derivatives was prepared as part of a search for subtype-selective human peroxisome proliferator-activated receptor (PPAR) activators. Structure-activity relationship studies indicated that the substituent at the alpha-position of the carboxyl group plays a key role in determining the potency and the selectivity for PPAR transactivation.
authors.affiliation: Discovery Research Laboratories, Kyorin Pharmaceutical Co., Ltd., 2399-1Mitarai, Nogi-machi, Shimotsuga-gun, 329-0114, Tochigi, Japan. hiroyuki.miyachi@mb2.kyorin-pharm.co.jp
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Miyachi
authors.forename: Masahiro
authors.initials: M
authors.lastname: Nomura
authors.forename: Takahiro
authors.initials: T
authors.lastname: Tanase
authors.forename: Yukie
authors.initials: Y
authors.lastname: Takahashi
authors.forename: Tomohiro
authors.initials: T
authors.lastname: Ide
authors.forename: Masaki
authors.initials: M
authors.lastname: Tsunoda
authors.forename: Koji
authors.initials: K
authors.lastname: Murakami
authors.forename: Katsuya
authors.initials: K
authors.lastname: Awano
mesh_terms: D000818:Animals; D019556:COS Cells; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D017930:Genes, Reporter; D006801:Humans; D010666:Phenylpropionates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020033:Protein Isoforms / Q000819:agonists; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists*; D013329:Structure-Activity Relationship; D014157:Transcription Factors / Q000819:agonists*; D015533:Transcriptional Activation / Q000187:drug effects; D014162:Transfection
chemical_list: D010666:Phenylpropionates; D020033:Protein Isoforms; D018160:Receptors, Cytoplasmic and Nuclear; D014157:Transcription Factors