吡啶 -2- 丙酸类：作为抗糖尿病药物的双效过氧化物酶体增殖物激活受体α/γ激动剂的发现。
Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
作者信息
Humphries Paul S, Almaden Jonathon V, Barnum Sandra J, Carlson Thomas J, Do Quyen-Quyen T, Fraser James D, Hess Mary, Kim Young H, Ogilvie Kathleen M, Sun Shaoxian
机构信息
Department of Diabetes Chemistry, Pfizer Global R&D, 10770 Science Center Drive, San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2006 Dec 1;16(23):6116-9. doi: 10.1016/j.bmcl.2006.08.105. Epub 2006 Sep 18.
A series of novel pyridine-2-propanoic acids was synthesized. A structure-activity relationship study of these compounds led to the identification of potent dual PPARalpha/gamma agonists with varied isoform selectivity. Based on the results of efficacy studies in diabetic (db/db) mice, and the desired pharmacokinetic parameters, compound (S)-13 was selected for further profiling.
合成了一系列新型吡啶 -2- 丙酸。对这些化合物的构效关系研究导致鉴定出具有不同亚型选择性的强效双PPARα/γ激动剂。基于在糖尿病（db/db）小鼠中的药效学研究结果以及所需的药代动力学参数，选择化合物（S）-13进行进一步分析。
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