茚满二酮衍生物：过氧化物酶体增殖物激活受体γ（PPARγ）激动剂的新型模板。
Indenone derivatives: a novel template for peroxisome proliferator-activated receptor gamma (PPARgamma) agonists.
作者信息
Ahn Jin Hee, Shin Mi Sik, Jung Sun Ho, Kang Seung Kyu, Kim Kwang Rok, Rhee Sang Dal, Jung Won Hoon, Yang Sung Don, Kim Seung Jun, Woo Joo Rang, Lee Jeong Hyung, Cheon Hyae Gyeong, Kim Sung Soo
机构信息
Bioorganic Science Division, Korea Research Institute of Chemical Technology, Yuseong-Gu, Daejeon, 305-600, Republic of Korea.
出版信息
J Med Chem. 2006 Jul 27;49(15):4781-4. doi: 10.1021/jm060389m.
Agonists of peroxisome proliferator-activated receptor gamma (PPAR gamma) are of interest as a treatment for diabetes, which prompted the identification of a new class of non-TZD PPAR gamma agonist. Moreover, compound 14c has displayed the most active agonistic activity with an EC50 value of 50 nM, in addition to exhibiting a new binding mode in the X-ray cocrystal structure.
过氧化物酶体增殖物激活受体γ（PPARγ）激动剂作为糖尿病的一种治疗手段备受关注，这促使了一类新型非噻唑烷二酮类PPARγ激动剂的发现。此外，化合物14c表现出最活跃的激动活性，其半数有效浓度（EC50）值为50 nM，并且在X射线共晶体结构中呈现出一种新的结合模式。
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