Pyridine-3-propanoic acids: Discovery of dual PPARα/γ agonists as antidiabetic agents

…, S Bailey, JV Almaden, SJ Barnum, TJ Carlson…

文献索引：Humphries, Paul S.; Bailey, Simon; Almaden, Jonathon V.; Barnum, Sandra J.; Carlson, Thomas J.; Christie, Lance C.; Do, Quyen-Quyen T.; Fraser, James D.; Hess, Mary; Kellum, Jack; Kim, Young H.; McClellan, Guy A.; Ogilvie, Kathleen M.; Simmons, Brett H.; Skalitzky, Donald; Sun, Shaoxian; Wilhite, David; Zehnder, Luke R. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 23 p. 6120 - 6123

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被引用次数: 10

摘要

A series of novel pyridine-3-propanoic acids was synthesized. A structure–activity relationship study of these compounds led to the identification of potent dual PPARα/γ agonists with varied isoform selectivity. Based on the results of efficacy studies in diabetic (db/db) mice, and the desired pharmacokinetic parameters, compounds (S)-14 and (S)-19 were selected for further profiling.