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Jung, Sang Hoon,Park, Soo Young,Kim-Pak, Youngmi,Lee, Hong Kyu,Park, Kyong Soo,Shin, Kuk Hyun,Ohuchi, Kazuo,Shin, Hyun-Kyung,Keum, Sam Rok,Lim, Soon Sung The Pharmaceutical Society of Japan 2006 Chemical & pharmaceutical bulletin Vol.54 No.3
<P>Fifteen chalcones and three thiazolidinedione (TZD) chalcones were prepared to evaluate their peroxisome proliferator-activated receptor-γ (PPAR-γ) ligand-binding activities. Among the three TZDs, one compound possessed PPAR-γ transactivation potential, while the others showed antagonistic activity against PPAR-γ 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-γ activation.</P>