Effect of Stilbene and Chalcone Scaffolds Incorporation in Clofibric Acid on PPARα Agonistic Activity
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In an effort to develop safe and efficacious compounds for the treatment of metabolic disorders, new compounds based on a combination of clofibric acid, the active metabolite of clofibrate, and trans-stilbene, chalcone, and other lipophilic groups were synthesized. They were evaluated for PPARα transactivation activity; all branched derivatives showed an increase of the transcriptional activity of receptor compared to the linear ones. Noteworthy, stilbene and benzophenone branched derivatives activated the PPARα better than clofibric acid.
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Tesse G, Tolomeo A, De Filippis B, Giampietro L Molecules. 2024; 29(17).
PMID: 39275108 PMC: 11396893. DOI: 10.3390/molecules29174260.
Lin C, Sun G, Li Y RSC Med Chem. 2024; 15(7):2413-2421.
PMID: 39026637 PMC: 11253847. DOI: 10.1039/d3md00727h.
Linciano P, Quotadamo A, Luciani R, Santucci M, Zorn K, Foil D J Med Chem. 2023; 66(22):15230-15255.
PMID: 37921561 PMC: 10683024. DOI: 10.1021/acs.jmedchem.3c01322.
Linciano P, De Filippis B, Ammazzalorso A, Amoia P, Cilurzo F, Fantacuzzi M Medchemcomm. 2020; 10(11):1892-1899.
PMID: 32206235 PMC: 7069374. DOI: 10.1039/c9md00286c.
Ammazzalorso A, Carradori S, Angeli A, Akdemir A, De Filippis B, Fantacuzzi M J Enzyme Inhib Med Chem. 2019; 34(1):1051-1061.
PMID: 31074307 PMC: 6522927. DOI: 10.1080/14756366.2019.1611801.