Design and synthesis of substituted phenylpropanoic acid derivatives as human peroxisome proliferator-activated receptor alpha/delta dual agonists.

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Kasuga J, Makishima M, Hashimoto Y, Miyachi H

Design and synthesis of substituted phenylpropanoic acid derivatives as human peroxisome proliferator-activated receptor alpha/delta dual agonists.

Bioorg Med Chem Lett. 2006 Feb;16(3):554-8. Epub 2005 Nov 3.

PubMed ID

16275077 [ View in PubMed

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Abstract

A series of phenylpropanoic acids was prepared as candidate dual agonists of peroxisome proliferator-activated receptors (PPAR) alpha and delta. Structure-activity relationship studies indicated that the shape of the linker moiety and the nature of the substituent at the distal benzene ring play key roles in determining the potency and selectivity of PPAR subtype transactivation. Optically active alpha-ethylphenylpropanoic acid derivatives were identified as potent human PPAR alpha and delta dual agonists with potential for the treatment of metabolic syndrome.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
(2S)-2-{3-[({[2-fluoro-4-(trifluoromethyl)phenyl]carbonyl}amino)methyl]-4-methoxybenzyl}butanoic acid	Peroxisome proliferator-activated receptor delta	EC 50 (nM)	12	N/A	N/A	Details