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
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container_issue 1
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container_title Bioorganic & medicinal chemistry letters
container_volume 12
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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