Synthesis and PPAR-gamma ligand-binding activity of the new series of 2'-hydroxychalcone and thiazolidinedione derivatives

Chemical & Pharmaceutical Bulletin
Sang Hoon JungSoon Sung Lim

Abstract

Fifteen chalcones and three thiazolidinedione (TZD) chalcones were prepared to evaluate their peroxisome proliferator-activated receptor-gamma (PPAR-gamma) ligand-binding activities. Among the three TZDs, one compound possessed PPAR-gamma transactivation potential, while the others showed antagonistic activity against PPAR-gamma transactivation. Among the chalcones, compound 5 was the most potent, and structure-activity relationship studies indicated that a methoxyl group in position C-4 and hydroxyl group in position C-4' or 5' in chalcone plays a key role in determining the potency of PPAR-gamma activation.

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Citations

Oct 10, 2013·Journal of Enzyme Inhibition and Medicinal Chemistry·Ming-Xia SongHu-Ri Piao
Nov 28, 2012·Chemical & Pharmaceutical Bulletin·Jason Taylor SchottHubrecht Johan Peter de Lijser
Jan 15, 2016·Bioorganic & Medicinal Chemistry·Emily HofmannStefan Paula
Apr 4, 2014·Organic & Biomolecular Chemistry·Fang-Wu WangJun-Ying Miao
Oct 3, 2018·Current Medicinal Chemistry·Sonia RochaMarisa Freitas
Jul 31, 2007·Biochemical and Biophysical Research Communications·Meryl HassanMarie-Josèphe Amiot
Nov 7, 2021·Scientific Reports·Emelda N OkoloOguejiofo T Ujam

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