AI Article Synopsis
- A series of 3-(4-alkoxyphenyl)propanoic acid derivatives were developed to selectively activate PPAR delta, inspired by the dual agonist TIPP-401.
- Research highlighted that the length of the alkoxy chain at the 4-position is crucial, with the n-butoxy variant showing the strongest PPARdelta activity and selectivity.
- A specific (S)-enantiomer demonstrated potent transactivation similar to or better than the well-known GW-501516, suggesting its potential as a drug for metabolic syndrome treatment by influencing lipid and glucose regulation.
Article Abstract
A series of 3-(4-alkoxyphenyl)propanoic acid derivatives was prepared as candidate peroxisome proliferator-activated receptor (PPAR) delta-selective agonists, based on our previously discovered potent human PPARalpha/delta dual agonist TIPP-401 as a lead compound. Structure-activity relationship studies clearly indicated the importance of the chain length of the alkoxy group at the 4-position, and the n-butoxy compound exhibited the most potent PPARdelta transactivation activity and highest PPARdelta selectivity. The (S)-enantiomer of a representative compound exhibited extremely potent PPARdelta transactivation activity, comparable with or somewhat superior to that of the known PPARdelta-selective agonist, GW-501516. The representative compound regulated the expression of genes involved in lipid and glucose homeostasis, and should be useful not only as a chemical tool to study PPARdelta function, but also as a candidate drug for the treatment of metabolic syndrome.
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| http://dx.doi.org/10.1016/j.bmc.2007.05.023 | DOI Listing |
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