Design, synthesis and evaluation of substituted phenylpropanoic acid derivatives as peroxisome proliferator-activated receptor (PPAR) activators: novel human PPARalpha-selective activators.
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.
Miyachi
Hiroyuki
H
Discovery Research Laboratories, Kyorin Pharmaceutical Co., Ltd., 2399-1Mitarai, Nogi-machi, Shimotsuga-gun, 329-0114, Tochigi, Japan. hiroyuki.miyachi@mb2.kyorin-pharm.co.jp
Nomura
Masahiro
M
Tanase
Takahiro
T
Takahashi
Yukie
Y
Ide
Tomohiro
T
Tsunoda
Masaki
M
Murakami
Koji
K
Awano
Katsuya
K
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
D010666:Phenylpropionates; D020033:Protein Isoforms; D018160:Receptors, Cytoplasmic and Nuclear; D014157:Transcription Factors