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...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2002-01, Vol.12 (1), p.77-80
Hauptverfasser:	Miyachi, Hiroyuki, Nomura, Masahiro, Tanase, Takahiro, Takahashi, Yukie, Ide, Tomohiro, Tsunoda, Masaki, Murakami, Koji, Awano, Katsuya
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals COS Cells Drug Design Drug Evaluation, Preclinical Genes, Reporter Humans Phenylpropionates - chemical synthesis Phenylpropionates - chemistry Phenylpropionates - pharmacology Protein Isoforms - agonists Receptors, Cytoplasmic and Nuclear - agonists Structure-Activity Relationship Transcription Factors - agonists Transcriptional Activation - drug effects Transfection
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Zusammenfassung:	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.
ISSN:	0960-894X