Design, synthesis and evaluation of substituted phenylpropanoic acid derivatives as peroxisome proliferator-activated receptor (PPAR) activators: novel human PPARalpha-selective activators.

Article Details

Citation

Miyachi H, Nomura M, Tanase T, Takahashi Y, Ide T, Tsunoda M, Murakami K, Awano K

Design, synthesis and evaluation of substituted phenylpropanoic acid derivatives as peroxisome proliferator-activated receptor (PPAR) activators: novel human PPARalpha-selective activators.

Bioorg Med Chem Lett. 2002 Jan 7;12(1):77-80.

PubMed ID
11738577 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
BezafibratePeroxisome proliferator-activated receptor alphaEC 50 (nM)>78000N/AN/ADetails
BezafibratePeroxisome proliferator-activated receptor gammaEC 50 (nM)>137000N/AN/ADetails