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 |
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creator | Miyachi, Hiroyuki Nomura, Masahiro Tanase, Takahiro Takahashi, Yukie Ide, Tomohiro Tsunoda, Masaki Murakami, Koji Awano, Katsuya |
description | 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. |
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source | MEDLINE; Elsevier ScienceDirect Journals |
subjects | 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 |
title | Design, synthesis and evaluation of substituted phenylpropanoic acid derivatives as peroxisome proliferator-activated receptor (PPAR) activators: novel human PPARalpha-selective activators |
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